P11149 is a competitive, BBB-penetarated weakly, orally active and selective inhibitor of AChE. P11149 exhibits an IC50 of 1.3 μM for rat BChE/AChE. P11149, a Galanthamine derivative, demonstrates central cholinergic activity, behavioral efficacy and safety. P11149 is used in the study for Alzheimer's disease.

PF-05221304 is an orally bioavailable, liver-directed and dual ACC1 (and ACC2) inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2, 12.4 nM for human ACC1 and 8.7 nM for human ACC2. PF-05221304 is a substrate for organic anion transport polyp

IYPTNGYTR, a deamidation-sensitive signature peptide, is a deamidation product of Trastuzumab. IYPTNGYTR can be used to monitor in vivo Trastuzumab metabolism.

FTISADTSK is an endogenous stable signature peptide from Trastuzumab monitored by selected reaction monitoring (SRM).

IYPTNGYTR acetate, a deamidation-sensitive signature peptide, is a deamidation product of Trastuzumab. IYPTNGYTR acetate can be used to monitor in vivo Trastuzumab metabolism.

FTISADTSK acetate is an endogenous stable signature peptide from Trastuzumab monitored by selected reaction monitoring (SRM).

L-Leucyl-L-Leucine methyl ester (LLOMe) hydrobromide, a dipeptide condensation product of L-leucine methyl ester generated by human monocytes or polymorphonuclear leukocytes, selectively eliminates lymphocytes with cytotoxic potential. L-Leucyl-L-Leucine

D-Ribose 5-phosphate disodium dihydrate is an intermediate of the oxidative branch of the pentose phosphate pathway (PPP) and an end product of the nonoxidative branch of the PPP. D-Ribose 5-phosphate is used in the synthesis of nucleotides and nucleic ac

Gamma-glutamylcysteine (γ-Glutamylcysteine), a dipeptide containing cysteine and glutamic acid, is a precursor to glutathione (GSH). Gamma-glutamylcysteine is a cofactor for glutathione peroxidase (GPx) to increase GSH levels.

5β-Dihydrocortisone is a sterol metabolite of cortisone by 5β-reductase (AKR1D1) in liver.

FTI-2153 TFA is a potent and highly selective inhibitor of farnesyltransferase (FTase), with an IC50 of 1.4 nM. FTI-2153 TFA is >3000-fold more potent at blocking H-Ras (IC50, 10 nM) than Rap1A processing. Anti-cancer activity.

trans-Chalcone, isolated from Aronia melanocarpa skin, is a biphenolic core structure of flavonoids precursor. trans-Chalcone is a potent fatty acid synthase (FAS) and α-amylase inhibitor. trans-Chalcone causes cellcycle arrest and induces apoptosis in th

GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 quarterhydrate stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 quarterhydrate shows significant glucose lowering in high fat fed fe

Uralenol is a natural PTP1B inhibitor (IC50=21. 5 μM) from Broussonetia papyrifera. PTP1B have been shown to play a major role in the dephosphorylation of the insulin receptor in many cellular and biochemical studies.

Thioquinapiperifil dihydrochloride (KF31327), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study.

Thioquinapiperifil (KF31327 free base), a potent, selective and non-competitive phosphodiesterase-5 (PDE-5, IC50 of 0.074 nM) inhibitor, is used for sexual enhancement study.

PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5

Ilexoside O is a triterpene saponin isolated from the roots of Ilex pubescens. Ilexoside O exhibits weak xanthine oxidase (XOD) inhibitory activity (IC50=53.05 μM).

Enasidenib (Idhifa, AG-221) mesylate is an orally available, selective and potent inhibitor of mutant isocitrate dehydrogenase 2 (IDH2).

Isomalt (Palatinitol) is a sugar alcohol used as an excipient in commercially available solid oral dosage forms. Isomalt stabilizes lactate dehydrogenase (LDH) moderately during freeze-drying.

Iproniazid (Marsilid, Iprazid) phosphate is a non-selective, irreversible monoamine oxidase (MAO) inhibitor (MAOI) that is used as an antidepressive agent.

Pseudocoptisine (Isocoptisine) chloride is a quaternary alkaloid with benzylisoquinoline skeleton, was isolated from Corydalis Tuber. Pseudocoptisine chloride inhibits acetylcholinesterase (AChE) activity with an IC50 of 12.8 μM. Anti-inflammatory and ant

Vardenafil (BAY38-9456, Levitra, Staxyn) hydrochloride is a selective, orally active, potent inhibitor of phosphodiesterase (PDE) with IC50 of 0.7 nM, 11 nM and 180 nM for PDE5, PDE6 and PDE1, respectively.

O-Desmethyl Galanthamine (Sanguinine) is galanthamine-type alkaloid. O-Desmethyl Galanthamine is an acetylcholinesterase (AChE) inhibitor, with an IC50 1.83 μM.

TIP 39, Tuberoinfundibular Neuropeptide is a neuropeptide and parathyroid hormone 2 receptor (PTH2R) agonist. TIP 39 is highly conserved among species. TIP39 from all species activates adenylyl cyclase and elevates intracellular calcium levels through parathyroid hormone 2 receptor (PTH2R).

NMNNAGDKWSAFLKEQSTLAQMYPLQEIQNLTVKLQLQALQQ is an angiotensin-converting enzyme 2 (ACE2) related peptide that can be used as a tool for understanding ACE2 functions.

Retagliptin (SP2086) is a selective, competitive and orally active dipeptidyl peptidase-4 (DPP-4) inhibitor. Retagliptin can be used for type 2 diabetes mellitus (T2DM) research.

16α-Hydroxyprednisolone is a stereoselective metabolite of the 22(R) epimer of the glucocorticoid budesonide via cytochrome P450 3A (CYP3A) enzymes.

Orotidine, a nucleotide, is an intermediate in pyrimidine nucleotide biosynthesis in RNA and DNA. Orotidine is mainly found in bacteria, fungi and plants.

OMDM-1 is a potent, selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki of 2.4 μM.

OMDM-2 is a potent, selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki of 3.0 μM.

Lysophosphatidylcholine 18:2 (1-Linoleoyl-2-Hydroxy-sn-glycero-3-PC), a lysophospholipid, is a potential biomarker identified from insulin resistance (IR) polycystic ovary syndrome (PCOS). Low plasma Lysophosphatidylcholine 18:2 also has been shown to predict impaired glucose tolerance, insulin resistance, type 2 diabetes, coronary artery disease, and memory impairment.

Sodium 3-methyl-2-oxobutanoate is a precursor of pantothenic acid in Escherichia coli.

3,5-Dimethylbenzaldehyde is a building block in the chemical synthesis.

Myristelaidic acid (trans-9-Tetradecenoic acid), a 14-carbon trans fatty acid, is the trans isomer of Myristoleic acid. Myristelaidic acid is found in most animal fats.

Taurohyodeoxycholic acid is the tauroconjugated form of Hyodeoxycholic acid (HDCA, a dihydroxylated natural bile acid). Taurohyodeoxycholic acid induces a biliary phospholipid secretion and suggests a hepatoprotective potential. Taurohyodeoxycholic acid also can promote gallstone dissolution.

Alkaline phosphatase is a membrane-bound glycoprotein that catalyzes the hydrolysis of phosphate monoesters at basic pH values. Alkaline phosphatase can be used for molecular biology and enzyme immunoassay.

Tangshenoside I, isolated from the roots of Codonopsis lanceolata, exhibits weak α-glucosidase inhibitory activities in vitro with an IC50 of 1.4 mM.

Guanylate cyclase-IN-1 (Example 46) is a guanylate cyclase inhibitor that can be used for cardiovascular diseases research.

Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) is a potent and direct inhibitor of 5-LO (5-Lipoxygenase) that reduces 5-LO activity in cell-free assays. CDC also inhibits 12-LO and 15-LO.

N-Arachidonyl maleimide is a potent, irreversible inhibitor of monoacylglycerol lipase (MAGL) with an IC50 value of 140 nM.

Glicoricone, a phenolic compound, is isolated from a species of licorice. Glicoricone is an inhibitor of monoamine oxidase (MAO), with an IC50 of 140 μM. Glicoricone binds to estrogen receptor (ER) and shows estrogen antagonist activity.

CCT129957 is an indole derivative and a potent phospholipase C-γ (PLC-γ) inhibitor with an IC50 of ~3 μM and a GC50 of 15 μM. CCT129957 inhibits Ca2+ release in squamous carcinoma cells at ~15 μM.

DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property.

Handle region peptide, rat is a prorenin receptor antagonist, suppresses the progression of diabetic nephropathy and has anti-inflammatory in the eye.

3-O-Ethyl-L-ascorbic acid, a stable vitamin C derivative, is a cosmetic tyrosinase tnhibitor with a whitening capacity. 3-O-Ethyl-L-ascorbic acid also has antioxidant abilities.

N-Acetyloxytocin is isolated and characterized in the neurointermediate lobe of the rat pituitary (NIL) and their presence in several brain areas of the rat.

(R)-MLN-4760, the R-enantiomer of MLN-4760, is a potent and selective ACE2 inhibitor, with an IC50 of 0.44 nM for human ACE2. (R)-MLN-4760 shows more than 5000-fold selectivity for ACE2 over ACE (IC50>100 μM) and CPDA (IC50=27 μM).

Troleandomycin (Triacetyloleandomycin), a macrolide acrolide antibiotic, is a selective CYP3A inhibitor.

Cyanidin 3-arabinoside is a selective and reversible protein tyrosine phosphatase 1B (PTP1B) inhibitor, with an IC50 of 8.91 μM. Cyanidin 3-arabinoside is potential for the research of type 2 diabetes.

2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one is a natural product found in the leaves and stem bark of M. glabra. 2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one displays binding affinities with dipeptidyl peptidase-4 (DPP-4) and α-Amylase. 2-Methoxy-5-acetoxy-fruranogermacr-1(10)-en-6-one has potential antidiabetic activities.

3-O-Acetyl-11-hydroxy-beta-boswellic acid is a potent 5-lipoxygenase (5-LO) inhibitor.

UK122 is a potent and selective urokinase-type plasminogen activator (uPA) inhibitor with an IC50 of 0.2 μM. UK122 shows no or little inhibition of tissue-type PA (tPA), plasmin, thrombin, and trypsin (all IC50>100 μM). UK122, 4-oxazolidinone analogue, is an anticancer agent and inhibits cancer cell migration and invasion.

Iso-Sagittatoside A is the metabolite of effective Erxian Decoction (EXD, a Chinese medicine prescription for menopausal syndromes) in rat plasma.

(+)-Medioresinol Di-O-β-D-glucopyranoside is a lignan glucoside with strong inhibitory activity of 3', 5'-cyclic monophosphate (cyclic AMP) phosphodiesterase.

5-Feruloylquinic acid (5-FQA) possesses antioxidative effects and tyrosinase inhibitory activities.

19α-Hydroxyasiatic acid, a natural triterpenoid, possesses anti-elastase activity.

Bisabolone oxide A is an α-glucosidase inhibitor.

Broussoflavonol F possess xanthine oxidase inhibitory activity.

Protamine sulfate, polycationic peptide and a antiheparin agent, could neutralize the anticoagulant action of heparin and enhances lipid-mediated gene transfer.

Liarozole (R75251; R85246) is an imidazole derivative and a retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.

AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease.

Trans-4-Phenyl-3-buten-2-one (trans-Benzylideneacetone, trans-Benzalacetone, trans-Benzylideneacetone) is an inhibitor of the enzyme phospholipase A2 (PLA2). Trans-4-Phenyl-3-buten-2-one is used as a flavouring agent, a fragrance and a bacterial metabolite.

SCD1 inhibitor-3 is a safe, potent and orally active SCD1 inhibitor. SCD1 inhibitor-3 can be used for the research of metabolic diseases such as obesity, type II diabetes and dyslipidemia, as well as skin diseases, acne and cancer.

DUN41875, also known as SCD1 inhibitor-4, is a potent, orally active stearoylCoA desaturase-1 (SCD1) inhibitor. SCD1 inhibitor-4 can be used for the research of diabetes. DUN41875 was first reported in Bioorgan.Med. Chem. Lett. (2011), 21(6), 1621-1625. This product has no formal name at the moment. For the convenience of communication, a temporal code name was therefore proposed according to MedKoo Chemical Nomenclature 

Kaempferol 3,4'-diglucoside is a flavonol isolated from the aqueous methanolic extract of norway spruce buds. Kaempferol 3,4'-diglucoside is identified in the needles.

Mevalonic acid 5-pyrophosphate (5-Diphosphomevalonic acid) tetralithium is an endogenous metabolite of the mevalonate pathway.

Creatine D3 hydrate is a deuterium labeled Creatine hydrate. Creatine hydrate is pivotal in energy metabolism of muscle and brain cells, both in physiological and in pathological conditions.

2'-Deoxyuridine 5'-monophosphate disodium is reductively methylated to dTMP (2'-deoxythymidine 5'-monophosphate) by bisubstrate enzyme thymidylate synthase (TS). dTMP is a nucleotide required for DNA synthesis.

2'-Deoxyguanosine 5'-monophosphate disodium (5′-dGMP disodium) is a mononucleotide having guanine as the nucleobase. 2'-Deoxyguanosine 5'-monophosphate disodium is a nucleic acid guanosine triphosphate (GTP) derivative.

2′-Deoxyadenosine 5′-monophosphate disodium, a nucleic acid AMP derivative, is a deoxyribonucleotide found in DNA. 2′-Deoxyadenosine 5′-monophosphate disodium can be used to study adenosine-based interactions during DNA synthesis and DNA damage.

ACAT-IN-2 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 187. ACAT-IN-2 inhibits NF-κB mediated transcription.

ACAT-IN-3 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-3 inhibits NF-κB mediated transcription.

ACAT-IN-4 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-4 inhibits NF-κB mediated transcription.

ACAT-IN-5 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-5 inhibits NF-κB mediated transcription.

ACAT-IN-6 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 200. ACAT-IN-6 potently inhibits NF-κB mediated transcription.

ACAT-IN-7 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-7 inhibits NF-κB mediated transcription.

ACAT-IN-8 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor. ACAT-IN-8 inhibits NF-κB mediated transcription.

ACAT-IN-9 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 207. ACAT-IN-9 inhibits NF-κB mediated transcription.

ACAT-IN-10 is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 197. ACAT-IN-10 weakly inhibits NF-κB mediated transcription.

ACAT-IN-10 dihydrochloride is an acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor extracted from patent EP1236468A1, example 197. ACAT-IN-10 dihydrochloride weakly inhibits NF-κB mediated transcription.

Polyphyllin C (compound 2) is a spirostanol saponin. Polyphyllin C exhibits mild (IC50=36.87 µM) activities against the tyrosinase and moderate (IC50=1.59 µg/mL) antileishmanial activities.

Benzolamide (CL11366) is a potent carbonic anhydrase (CA) inhibitor, with Kis of 15 nM, 9 nM, 94 nM and 78 nM for hCA I, hCA II, EcoCAγ and VchCAγ, respectively. Benzolamide also inhibits CAS3, with a Ki of 54 nM. Benzolamide can be used for the research of glaucoma and seizures.

Dapaconazole, as an antifungal agent, inhibits sterol 14α-demethylase cytochrome P450 activity with an IC50 of 1.4 μM.

Manoalide is a potent Phospholipase A2 (PLA2) and Phospholipase C (PLC) inhibitor. Manoalide, a sesterpenoid compound, displays anti-inflammatory and antibacterial activities.

OBAA is a potent phospholipase A2 (PLA2) inhibitor with an IC50 of 70 nM. OBAA blocks Melittin-induced Ca2+ influx in Trypanosoma brucei with an IC50 of 0.4 μM.

Myrciacetin is a flavonoid from Rhododendron dauricum. Myrciacetin is against rat lens aldose reductase with an IC50 of 13 μM.

WT IDH1 Inhibitor 2 is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. WT IDH1 Inhibitor 2 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity.

LDHA-IN-3, as a selenobenzene compound, is a potent, noncompetitive lactate dehydrogenase (LDHA) inhibitor (IC50=145.2 nM). LDHA-IN-3 can be used for the research of cancer.

Isolindleyin, a butyrophenone, is a tyrosinase inhibitor, with a Kd of 54.8 μM for human tyrosinase. Isolindleyin exhibits anti-inflammatory, analgesic and anti-melanogenic activities.

7-Methylguanosine 5'-diphosphate (7-Methyl-GDP) sodium, a cap analog, can be used in the synthesis of mRNA cap analogues.

Camellianin B, a flavonoid compound, is a Camellianin A metabolite. Camellianin B has antioxidant and angiotensin converting enzyme (ACE) inhibitory activities.

CP-610431 is a reversible, ATP-uncompetitive, isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor. CP-610431 inhibits ACC1 and ACC2 with IC50s of ~50 nM. CP-610431 can be used for the research of metabolic syndrome.

4-Hydroxyphenylbutazone is a metabolite of Phenylbutazone. Phenylbutazone, a nonsteroidal anti-inflammatory drug (NSAID), is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS).

16α-Hydroxyestrone (16αOHE) is a major Estradiol metabolite. 16α-Hydroxyestrone (16αOHE) can be used for the research of metabolic disease.

Kaempferol-3,7-di-O-β-glucoside (Kaempferol 3,7-diglucoside), a flavonol, possesses enzyme inhibition property towards α-amylase, α-glucosidase and Acetylcholinesterase. Kaempferol-3,7-di-O-β-glucoside protects differentiating neuronal cells, SH-SY5Y from Amyloid β peptide-induced injury. Kaempferol-3,7-di-O-β-glucoside has the potential for Alzheimer's research.

Lacto-N-biose I (Galβ1-3GlcNAc), as an endogenous metabolite, is an acceptor for the α1,2-fucosyltransferase enzyme from Helicobacter pylori.

S-(5'-Adenosyl)-L-methionine iodide (S-Adenosyl-L-methionine iodide) is an important methyl donor that is found in all living organisms.

Viscumneoside III, a dihydroflavone O-glycoside, is a potent tyrosinase inhibitor with an IC50 of 0.5 mM. Viscumneoside III has anti-angina pectoris.

Manghaslin is a flavonoid glycoside with anti-inflammatory activities. Manghaslin shows inhibitory activity against AChE with an IC50 of 94.92 µM.

Zenarestat is a potent and orally active aldose reductase inhibitor. Zenarestat improves diabetic peripheral neuropathy in Zucker diabetic fatty rats.

S-Adenosyl-L-methionine D3 (S-Adenosyl methionine D3) is a deuterium labeled S-Adenosyl-L-methionine. S-Adenosyl-L-methionine is produced endogenously from methionine and ATP by action of the enzyme methionine adenosyltransferase and is an important orally active methyl group donor.

Geranylgeranyl pyrophosphate is a metabolite involved in protein geranylgeranylation. Geranylgeranyl pyrophosphate is the common precursor of  diterpenoids, for example, Paclitaxel. Geranylgeranyl pyrophosphate can be used for cancer research.

Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a 5-HT2C receptor agonist...

Echimidine N-oxide, a pyrrolizidine alkaloid, has acetylcholinesterase (AChE) inhibitory activity (IC50=0.347 mM).

Homoeriodictyol is a flavonoid metabolite of Eriocitrin in plasma and urine. Eriocitrin is a strong antioxidant agent.

Forsythoside F (Arenarioside) is a xanthine oxidase inhibitor and possesses antihyperuricemic effects in vivo.

Cassiaside is a naphthopyrone glucoside, shows mixed-type inhibition against BACE1 (IC50=4.45 μM; Ki=9.85 μM). Cassiaside possesses potential anti- Alzheimer's disease (AD) activity.

Sildenafil-d3 is deuterium labeled Sildenafil-d3. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.

Milvexian (BMS-986177), an effective antithrombotic agent, is an orally-bioavailable, reversible and direct inhibitor of human and rabbit factor XIa (FXIa) with Ki of 0.11, and 0.38 nM, respectively.

BMT-297376, the optimized Linrodostat, is a potent IDO1 inhibitor.

CAY10698 (compound 1) is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC50 of 5.1 μM. CAY10698 is inactive against 5-LOX, 15-LOX-1, 15-LOX-2 and COX-1/2.

FR-229934 is a PDE V inhibitor extracted from patent WO2019130052A1. FR-229934 can be used for the research of pulmonary arterial hypertension and erectile dysfunction.

Aliskiren D6 hemifumarate (CGP 60536 D6 hemifumarate) is a deuterium labeled Aliskiren hemifumarate. Aliskiren hemifumarate is a direct and orally active renin inhibitor with an IC50 of 1.5 nM.

SHP2 IN-1 (compound 13) is an allergic inhibitor of SHP2 (PTPN11), with an IC50 of 3 nM.

FFAGLDD is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.

FFAGLDD TFA is MMP9 selective cleavage peptides, which used for cytosolic delivery of Doxorubi-cin (DOX) and achieve temporally and spatially controlled slow drug delivery and release.

LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion.

N4-Acetylcytidine triphosphate is efficiently used as a substrate in T7 Polymerase-catalyzed in vitro transcription and can be incorporated into multiple templates.

4'-Hydroxy diclofenac D4 is the deuterium labeled 4'-Hydroxy diclofenac. 4'-Hydroxy diclofenac is an orally active metabolite of Diclofenac by cytochrome P450 2C9 (CYP2C9). 4'-Hydroxy diclofenac has anti-inflammatory and analgesic properties.

IDH-C227 is a potent and selective IDH1R132H inhibitor. IDH-C227 has anticancer effcts.

Vitamin K1 D7 (Phylloquinone D7) is the deuterium labeled Vitamin K1. Vitamin K1 a naturally occurring vitamin required for blood coagulation and bone and vascular metabolism.

Diaplasinin (PAI-749) is a plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 of 295 nm. Antithrombotic efficacy.

TDI-10229 is a potent and orally bioavailable inhibitor of soluble adenylyl cyclase (sAC, ADCY10). TDI-10229 displays nanomolar inhibition of sAC in both biochemical and cellular assays (IC50 of 195 nM) and exhibits mouse pharmacokinetic properties sufficient to warrant its use as an in vivo tool compound.

1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone, a quinolone alkaloid, is a diacylglycerol acyltransferase inhibitor and angiotensin II receptor blocker, with IC50s of 20.1 μM and 34.1 μM, respectively. 1-Methyl-2-[(4Z,7Z)-4,7-tridecadienyl]-4(1H)-quinolone shows potent anti-Helicobacter pylori activity with the MIC of 10 μg/mL.

Lyciumin A, a cyclic octapeptide, exhibits inhibitory activity on proteases, renin and angiotensin-converting enzyme. Lyciumin A can be used for the research of hypertension.

LYP-IN-1 is a potent, selective and specific LYP inhibitor with a Ki and an IC50 of 110 nM and 0.259 μM, respectively. LYP-IN-1 also has selectivity for a large panel of PTPs, such as SHP1 (IC50=5 μM) and SHP2 (IC50=2.5 μM). LYP-IN-1 exhibits highly efficacious cellular activity in T- and mast cells. LYP-IN-1 can be used for the study of autoimmune disorders.

β-Secretase Inhibitor II is a β-Secretase inhibitor. β-Secretase Inhibitor II is a simple tripeptide aldehyde (IC50=700 nM for inhibition of total Aβ and IC50=2.5 μM for Aβ1–42). β-Secretase Inhibitor II can be used for the research of Alzheimer's disease.

Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific cathepsin L (CTSL) inhibitor.

Tovinontrine (IMR-687) is a highly potent and selective phosphodiesterase-9 (PDE9) inhibitor specifically for the treatment of sickle cell disease. IC50s are 8.19 nM and 9.99 nM for PDE9A1 and PDE9A2, respectively.

BACE-1 inhibitor 2 is a potent and CNS permeable BACE-1 inhibitor with an IC50 of 1.5 nM in BACE-1 enzymatic assay.

PF-8380 hydrochloride is a potent autotaxin inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.

Methyl citrate is a Monoamine oxidase B (MAO-B) inhibitor (IC50=0.23 mM). Methyl citrate is isolated from the fruits of Opuntia ficus-indica var. saboten Makino.

Angiotensinogen (1-14), human TFA is a fragment of the renin substrate angiotensinogen. Angiotensinogen is naturally occurring substrate for renin and a precursor for all angiotensin peptides.

1-Methyl-2-undecyl-4(1H)-quinolone is a potent, irreversible and selective inhibitor of type B monoamine oxidase (MAO-B). 1-Methyl-2-undecyl-4(1H)-quinolone shows a selective inhibition of MAO-B activity with the IC50 and Ki values of 15.3 μM and 9.91 μM, respectively, but did not inhibit type A MAO (MAO-A) activity. Methyl-2-undecyl-4(1H)-quinolone, as a quinolone alkaloid, is isolated from fresh leaves and fruits of Evodia rutaecarpa HOOK. f. et THOMS.

BACE1-IN-5 (Compound 15) is a β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 of 9.1 nM, and also inhibits cellular amyloid-β (Aβ) with an IC50 of 0.82 nM. BACE1-IN-5 has a medicinal chemistry that improves hERG inhibition and P-gp efflux.

CP-544439 is a potent and orally active matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 0.75 nM.

Fucoidan, a biologically active polysaccharide, is an efficient inhibitor of α-amylase and α-glucosidase. Anticoagulant, antitumor, antioxidant and antisteatotic activities.

MM 419447, a linaclotide metabolite, is a guanylate cyclase-C agonist. MM 419447 has the potential for the research of the irritable bowel syndrome with constipation (IBS-C).

Doxorubicinol hydrochloride (13-Dihydroadriamycin hydrochloride) is a secondary alcohol metabolite of Doxorubicin.

Folitixorin (5,10-methylenetetrahydrofolate) is a cofactor and an analog of leucovorin. Folitixorin is a promising agent for modulation of 5-FU cytotoxicity in adjuvant cancer research.

MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain.

(Rac)-OSMI-1 is the racemate of OSMI-1. OSMI-1 is a cell-permeable O-GlcNAc transferase (OGT) inhibitor with an IC50 value of 2.7 μM. OSMI-1 inhibits protein O-linked N-acetylglucosamine (O-GlcNAcylation) in several mammalian cell lines without qualitatively altering cell surface N- or O-linked glycans.

Acotiamide D6 is a deuterium labeled Acotiamide. Acotiamide is an orally active and first-in-class gastroprokinetic agent for the treatment of functional dyspepsia.

NoxA1ds TFA is a potent and selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds TFA exhibits selectivity for NOX1 over NOX2, NOX4, NOX5 and xanthine oxidase. NoxA1ds TFA inhibits NOX1-derived O2- production in HT-29 human colon cancer cells. NoxA1ds TFA attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro.

OT-82 is a novel nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with average IC50s of 13.03   nM in non-HP cancer cells and 2.89   nM in HP cancer cells, respectively.

Senazodan (MCI 154) (hydrochloride), as a Ca2+ sensitiser, shows inhibition effect on PDE III.

Carbazeran (citrate), a potent phosphodiesterase inhibitor, is aldehyde oxidase substrate. Carbazeran (citrate) can be used for the research of metabolic disease.

NHC-triphosphate tetraammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form. NHC-triphosphate tetraammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.

NHC-triphosphate triammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) as a triphosphate form. NHC-triphosphate triammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA.

AA38-3 is a serine hydrolase (SH) inhibitor. AA38-3 can inhibit three SHs, ABHD6, ABHD11, and FAAH.

CRA-2059 hydrochloride is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).

Cathepsin D and E FRET Substrate acetate is a fluorogenic substrate for cathepsins D and E and not for B, H or L. The cleavage occurs at the Phe-Phe amide bond resul. Cathepsin D and E FRET Substrate is a valuable tool for routine assays and for mechanistic studies on cathepsins E and D.

Lonodelestat (POL6014) is a potent, orally active and selective peptide inhibitor of human neutrophil elastase (hNE).

Mosliciguat is a guanylate cyclase activator.

2,8-Dihydroxyadenine, an endogenous metabolite, can cause the formation of urinary crystals and kidney stones. 2,8-Dihydroxyadenine can be used to diagnose adenine phosphoribosyltransferase (APRT) deficiency.

3-Oxo-4,6-choladien-24-oic acid is an endogenous metabolite. 3-Oxo-4,6-choladien-24-oic acid exsists in the urine of patients with hepatobiliary disease.

Ebaresdax can inhibit peroxynitrite oxidation derived by SIN-1 and peroxynitrite mediated Cytotoxicity with IC50s of 3.7±0.80 and 0.13±0.02 uM, respectively.

Eriodictyol chalcone possesses both anti-aromatase and an anti-17β-HSD activity.

Larsucosterol is a cholesterol metabolite from the nuclei of normal human liver tissues, epigenetically regulates the transcription of proteins and enzymes involved in lipid synthesis, inflammation, and apoptosis.

Tigulixostat is a novel (indolyl)heteroarylcarboxylate derivatives effective as non-purine selective xanthine oxidase inhibitor, which lowers the production of uric acid.

Orismilast (LEO-32731) is a PDE4 inhibitor used for the research of inflammatory diseases.

Larsucosterol sodium is a cholesterol metabolite from the nuclei of normal human liver tissues, epigenetically regulates the transcription of proteins and enzymes involved in lipid synthesis, inflammation, and apoptosis.

SSAO inhibitor-1 is a semicarbazide-sensitive amine oxidase (SSAO) inhibitor. SSAO inhibitor-1 has anti-inflammatory activity and can be used for liver diseases research.

Deutarserine is a deuterium modified analog of endogenous D-serine (CTP 692), which is used in the research of adults with schizophrenia.

Triiodothyronine sulfate is the main metabolite of thyroid hormone triiodothyronine (T3). Triiodothyronine is an active form of thyroid hormone, which binds to β1 thyroid hormone receptor (TRβ1), and activates its activity.

CDC25B-IN-2 is a potent cdc25B inhibitor.

CRA-2059 is a highly specific and selective tryptase inhibitor, with a Ki of 620 pM for recombinant human tryptase-β (rHTβ).

Tilpisertib is a serine/threonine kinase inhibitor (WO2017007689).

IHVR-11029 is a small molecule inhibitor of ER α-glucosidases, with an EC50 of 0.09 μM.

Salsolidine hydrochloride, a tetrahydroisoquinoline alkaloid, acts as a stereoselective competitive MAO A (monoamine oxidase A) inhibitor.

BN82002 hydrochloride is a potent, selective and irreversible inhibitor of CDC25 phosphatase family. BN82002 hydrochloride inhibits CDC25A, CDC25B2, CDC25B3, CDC25C CDC25A, and 25C-cat with IC50 values of 2.4, 3.9, 6.3, 5.4, and 4.6 µM, respectively. BN82002 hydrochloride displays ~20-fold greater selectivity over CD45 tyrosine phosphatase.

Irsenontrine (E2027) is an orally active and selective phosphodiesterase 9 (PDE 9) inhibitor. Irsenontrine can be used for the research of neurological diseases.

Phosphoribosyl pyrophosphate (PRPP) pentasodium is an important metabolite required in the biosynthesis of purine and pyrimidine nucleotides, the amino acids histidine and tryptophan, and the cofactors NAD and NADP.

Ro 20-1724 (Ro 20-174) is a potent inhibitor of cAMP-specific phosphodiesterase (PDE4/PDE IV) with a Ki of 1930 nM. Neuroprotective effect.

Kynuramine, an endogenously occurring amine, is a fluorescent substrate and probe of plasma amine oxidase.

Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD).

Inclisiran (ALN-PCSsc) is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK-9. Inclisiran can be used for hyperlipidemia and cardiovascular disease (CVD) research.

SLN124 is a GalNac-siRNA targeting transmembrane serine protease 6 (Tmprss6). SLN124 is composed of a trimeric GalNAc ligand conjugated to TMPRSS6‐siRNA. SLN124 has the potential for an siRNA to restore hepcidin expression and normalise iron homeostasis in β‐thalassaemia.

Fitusiran (ALN-AT3SC), an small interfering RNA, specifically targets antithrombin (AT) messenger RNA to lower production of AT in the liver. Fitusiran increases thrombin generation and has the potential for the research of the hemophilia.

PCSK9-IN-2 is a novel small molecule inhibitor of PCSK9-LDLR protein–protein interaction (PPI) with an IC50 value of 7.57 μM.

D-Cl-amidine hydrochloride is a potent and highly selective PAD1 inhibitor. D-Cl-amidine is well-torelated with no significant toxicity.

N-Desmethyl Sildenafil (Desmethylsildenafil) is a major metabolite of Sildenafil. Sildenafil is a potent phosphodiesterase type 5 (PDE5) inhibitor.

PDE4-IN-3 is a novel and orally active PDE4 inhibitor with potent inhibitory affinity (IC50 = 4.2 nM).

PROTAC SHP2 degrader-1 is a potent and effective SHP2 degrader. PROTAC SHP2 degrader-1 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins and is also neddylation- and proteasome-dependent.

PTP1B-IN-13 is a selective PTP1B inhibitor targeting the allosteric site with an IC50 value of 1.59 μM.

PTP1B-IN-14 is a selective PTP1B inhibitor (IC50 = 0.72 μM) targeting the allosteric site.

Okadaic acid, a marine toxin, is an inhibitor of protein phosphatases (PP), including PP1 (IC50=15-50 nM), PP2A (IC50=0.1-0.3 nM), PP3 (IC50=3.7-4 nM), PP4 (IC50=0.1 nM), PP5 (IC50=3.5 nM), with a significantly higher affinity for PP2A. Okadaic acid increase of phosphorylation of a number of proteins by inhibiting PP, and acts a tumor promoter.

28-O-β-D-Glucopyranosyl pomolic acid is a urokinase plasminogen activator inhibitor with IC50 at 37.82 μM.

ACT001 is orally active PAI-1 inhibitor by inhibiting the phosphorylation of PI3K and AKT. ACT001 inhibits the phosphorylation of STAT3 and PD-L1 expression by directly binding to STAT3. ACT001, a fumarate salt form of Micheliolide, can cross the blood-brain barrier. ACT001 has potent anti-glioblastoma (GBM) activity and immunomodulatory effects.

Liarozole Dihydrochloride is identified as a modest inhibitor of P450 with IC50 of 2.2–6.0 μM and 260 nM for CYP26 and rat CYP17 respectively.

Mulberrofuran G protects ischemic injury-induced cell death via inhibition of NOX4-mediated ROS generation and ER stress. Mulberrofuran G shows moderate inhibiting activity of hepatitis B virus (HBV) DNA replication with the

MAO-B-IN-2 is a selective and competitive inhibitor of MAO-B and BChE with IC50 values of 0.51 and 7.00 μM, respectively.

(+)-Cinchonaminone shows monoamine oxidase (MAO) inhibitory activity.

Ladostigil (TV-3326) hemitartrate is a dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with an IC50 of 37.1 and 31.8 μM for MAO-B and AChE, reapectively. Ladostigil hemitartrate could increase cholinergic transmission, prevent the formation of ROS or their actions and be used for the research of depression and Alzheimer's disease.

(S)-Salsolidine is a weak monoamine oxidase (MAO) inhibitor (Ki=63 μM). The R enantiomer of Salsolidine is more potent than the S form (Ki=26 μM).

ADAM8-IN-1 is a potent ADAM8 inhibitor with an IC50 value of 73 nM.

IDO-IN-15 is an IDO1 inhibitor (IC50 < 0.51 nM).

IDO-IN-14 is an IDO inhibitor with an IC50 value of 0.6928 nM.

Ganoderlactone D shows inhibitory effects of yeast α-Glucosidase with IC50 values of 41.7 μM.