Zifcasiran is a hypoxia-inducible factor (HIF) synthesis reducer. Zifcasiran shows antitumor activities and can be used in advanced renal cell carcinoma research.

Mersalyl (Salirgan) is a potent vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 (HIF-1) inducer. Mersalyl induces VEGF and ENO1 mRNA expression. Mersalyl shows diuresis effects.

Taragarestrant (D-0502) is a potent, orally active estrogen receptor degrader. Taragarestrant has antiproliferative activity against estrogen receptor-positive breast cancer cell lines and has anticancer activity. Taragarestrant can be used for cancer research.

FERb 033 is a selective and potent ERβ agonist (Ki=7.1 nM, EC50=4.8 nM). FERb 033 shows 62-fold selectivity over ERα.

Tilpisertib fosmecarbil is a potent serine/threonine kinase inhibitor. Tilpisertib fosmecarbil has anti-inflammatory activity.

Bezeparsen is a PCSK9 synthesis inhibitor.

CP-113818 is a potent cholesterol acyltransferase (ACAT) inhibitor. CP-113818 can be used for the research of Alzheimer's disease.

S-Adenosyl-L-methionine (p-toluenesulfonate) is a naturally occurring molecule distributed to virtually all body tissues and fluids. S-Adenosyl-L-methionine takes parts in biochemical reactions involving enzymatic transmethylation, acting as a methyl group donor. S-Adenosyl-L-methionine can prevent mortality induced by Acetaminophen and acute and chronic lead poisoning in animals model. S-Adenosyl-L-methionine also possess antidepressant property.

Parathyroid hormone (PTH) is a circulating hormone comprised of 84 amino acids. Parathyroid hormone is produced in the parathyroid glands and acts primarily on bone and kidney to maintain extracellular calcium levels within normal limits. Parathyroid hormone can be used for osteoporosis research.

Guanosine 5'-diphosphate (GDP) sodium is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate sodium is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate sodium can be used in the research of inflammation, such as anemia of inflammation (AI).

Folinic acid (Leucovorin) disodium is a biological folic acid and is a forms of vitamin B9. Folinic acid disodium is generally administered along with Methotrexate (MTX) as a rescue agent to decrease MTX-induced toxicity. Folinic acid disodium and Sfluorouracil adjuvant chemotherapy shows effective in colon carcinoma.

Levofloxacin N-oxide is a minor metabolite of Levofloxacin. Levofloxacin N-oxide does not exhibit significantly genotoxic risks. Levofloxacin is an orally active antibiotic and is active against both Gram-positive and Gram-negative bacteria.

Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2.

MFI8 is a small molecule inhibitor of mitochondrial fusion.

DPTIP-prodrug 18 (P18) is a orally active and brain-penetrable prodrug of DPTIP. DPTIP-prodrug 18 is a potent nSMase2 inhibitor. DPTIP-prodrug 18 significantly inhibits IL-1β-induced EV (extracellular vesicle) release by inhibition of nSMase2 (neutral sphingomyelinase-2) activity. DPTIP-prodrug 18 can be used for brain injury research.

Avanafil (TA-1790) dibenzenesulfonate is a potent and selective phosphodiesterase-5 (PDE-5) inhibitor with IC50 values of 5.2 nM, 630 nM, 5700 nM, 6200 nM, 12000 nM, 27000 nM, 51000 nM and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil dibenzenesulfonate activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil dibenzenesulfonate inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Avanafil dibenzenesulfonate can be used for the research of erectile dysfunction and osteoporosis.

SCH-42354 is a potent, orally active neutral endopeptidase (NEP) inhibitor, is the pharmacologically active form of the prodrug SCH-42495. SCH-42354 inhibits the hydrolysis of NEP to enhance the activity of atrial natriuretic peptide (ANP). SCH-42354 inhibits hydrolysis of leu-enkephalin and ANF with IC50 values of 8.3 nM and 10.0 nM, respectively. SCH-42354 has antihypertensive activity.

Masoprocol (meso-Nordihydroguaiaretic acid) is a potent and orally active lipoxygenase inhibitor. Masoprocol shows antihyperglycemic activity. Masoprocol decreases the glucose concentration and hepatic triglyceride in vivo. Masoprocol has the potential for the research of type II diabetes.

Simvastatin acid (Tenivastatin) is an orally active HMG-CoA reductase (HMGCR) inhibitor. Simvastatin acid reduces indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin acid can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene.

Edoxaban (DU-176b) hydrochloride is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with Ki values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban hydrochloride exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban hydrochloride can be used for preventing thromboembolic disease research.

Phenylsulfamide (Compound 10) is a human carbonic anhydrase-II (hCA-II) inhibitor with a Kd of 45.50 μM and a Ki of 79.60 μM.

Disulfamide, an orally active diuretic, is a carbonic anhydrase inhibitor with the IC50 value of 0.07 μM. Disulfamide leads to diuresis by inhibiting carbonic anhydrase and preventing the reabsorption of sodium and bicarbonate in the proximal tubule.

Puliginurad (YL-90148) is a potent urate transporter (URAT) inhibitor. Puliginurad can be used for hyperuricemia and gout research.

Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC50 of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, cocaine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential treatment for multiple forms of drug abuse. Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis.

Tribendimidine is an orally active, broad-spectrum anthelmintic agent, with particularly high activity against A. lumbricoides and N. americanus. Tribendimidine is also an L-type nicotinic acetylcholine receptor (nAChR) agonist.

L-Homocysteic acid (L-HCA) is an endogenous excitatory amino acid that acts as a NMDA receptor agonist (EC50: 14 μM). L-Homocysteic acid is neurotoxic, and can be used in the research of neurological disorders.

L-Cysteine S-sulfate is a potent N-methyl-d-aspartate (NMDA) glutamatergic receptors agonist. L-Cysteine S-sulfate is the substrate for cystine lyase.

Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research.

IAB15 is a potent T-type calcium channel inhibitor. IAB15 can be used for epilepsy research.

IAA65 is a potent T-type calcium channel inhibitor with a IC50 value of 18.9 µM. IAA65 can be used for epilepsy research.