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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC75890 NIC-12 NIC-12 is a potent NLRP3 inhibitor. NIC-12 selectively reduces circulating IL-1ß levels in the LPS-endotoxemia mice model. NIC-12 inhibits NLRP3 inflammasome activation in mouse macrophages.
DC75891 Donetidine Donetidine (SK&F 93574) is an antagonist for histamine H2 receptor, that promotes histamine release in beagle dog models.
DC75892 Ainuovirine Ainuovirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). Ainuovirine inhibits HIV replication by non-competitively binding to HIV reverse transcriptase and blocking the reverse transcription process of viral RNA. Ainuovirine can be used for human immunodeficiency virus (HIV) type 1 infection.
DC75893 Idazoxan Idazoxan (RX 781094) is a potent antagonist of α2 adrenergic receptor (α2AR) and potential I2 imidazoline receptor agonist. Idazoxan can be used in the research of antidepression and schizophrenia. Idazoxan has oral bioactivity.
DC75894 Imazodan Imazodan is a selective inhibitor for phosphodiesterase III (PDE III), which increases myocardial contractility by blocking the cAMP degradation, and improves the contractile function of heart. Imazodan serves also as a peripheral vasodilator.
DC75895 Kanosamine Kanosamine (3-Amino-3-deoxyglucose) is an antibiotic against Saccharomyces cerevisiae and human pathogenic fungi Candida albicans. Kanosamine exhibits antifungal activity through inhibition of cell wall synthesis and inhibition of GlcN-6-P synthase with phosphorylated kanosamine-6-phosphate in cytoplasma.
DC75896 Pelacarsen sodium Pelacarsen sodium is a liver-specific antisense oligonucleotide against apolipoprotein(a) that reduces lipoprotein(a) up to 80% with good tolerability.
DC75897 3-Nitrobenzoic acid 3-Nitrobenzoic acid (m-Carboxynitrobenzene; m-Nitrobenzenecarboxylic acid; m-Nitrobenzoic acid) is a strong antioxidant and antimicrobial agent that can inhibit the generation of free radicals and kill bacteria and fungi. 3-Nitrobenzoic acid is a kind of biological materials or organic compounds that are widely used in life science research.
DC75898 Amelparib hydrochloride Amelparib (JPI-289) hydrochloride is a potent, orally active, and water-soluble inhibitor of PARP-1. Amelparib hydrochloride inhibits PARP-1 activity (IC50 = 18.5 nM) and cellular PAR formation (IC50 = 10.7 nM). Amelparib hydrochloride is a potential neuroprotective agent. Amelparib hydrochloride has the potential for the research of acute ischaemic stroke.
DC75899 Aminocaproyl-Val-Cit-PABC-MMAE Aminocaproyl-Val-Cit-PABC-MMAE is an Drug-linker conjugate for ADC.
DC75900 MRS 2211 sodium hydrate MRS 2211 sodium hydrate is a competitive P2Y13 receptor antagonist (pIC50= 5.97). MRS 2211 sodium hydrate is highly selective to the P2Y13 receptor, showing more than 20-fold selectivity compared to the P2Y1 and P2Y12 receptors. MRS 2211 sodium hydrate can be used to further investigate the role of the P2Y13 receptor in different physiological and pathological processes, such as its function in blood cells, the nervous system and the immune system.
DC75901 Sulfaperin Sulfaperin (Methylsulfadiazin) is an antibacterial agent.
DC75902 SJH1-51B SJH1-51B is a potent PROTAC degrader of BRD4. SJH1-51B has anti-tumor effect.
DC75903 ZG-126 ZG-126 is an agonist for vitamin D receptor (VDR) and an inhibitor for histone deacetylase (HDAC) (IC50=0.63-67.6 μM). ZG-126 exhibits cytotoxicity in cancer cells MDA-MB-231 and 4T1. ZG-126 exhibits antitumor and anti-metastatic efficacy against melanoma and triple-negative breast cancer (TNBC) in mouse models. ZG-126 also exhibits anti-inflammatory activity, through the reduction of macrophage infiltration and immunosuppressive M2-polarization.
DC75904 ADS031 ADS031, a histamine H3R antagonist, displays 12.5 nM affinity at the hH3R and the highest inhibitory activity against AChE (IC50 = 1.537 μM).
DC75905 CLZX-205 CLZX-205 (compound C-7) is a selective inhibitor of CDK9, with the IC50 of 2.9 nM. CLZX-205 plays an important role in cancer research.
DC75906 TPA-NAC TPA-NAC is a nonfluorogenic prodrug by introducing N-acetyl-L-cysteine (NAC) into a conjugated acceptor skeleton. TPA-NAC is capable of fluorogenic selective labeling of HSA.
DC75907 CW2158 CW2158 (Compound 13) is a modulator for exportin1 (XPO1) ,which disrupts the chromatin binding, inhibits NFAT transcription factors and activation of T cells.
DC75908 Crenolanib benzenesulfonate Crenolanib benzenesulfonate is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
DC75909 Delucemine Delucemine is a selective serotonin reuptake inhibitor (SSRI) and NMDAR antagonist. Delucemine can be used as an antidepressant.
DC75910 Velnacrine Velnacrine (HP 029 free base) is an inhibitor for acetylcholinesterase (AChE), with an IC50 of 3.27 μM. Velnacrine reverses the Scopolamine-induced amnesia in rat models, and exhibits acute toxicity with LD50 of 65 mg/kg.
DC75911 SUN-1334H free base SUN-1334H free base is an orally active inhibitor for histamine H1 receptor, with an IC50 of 20.3 nM and Ki of 9.7 nM. SUN-1334H free base inhibits histamine-induced contractions of isolated guinea-pig ileum with an IC50 of 0.198 μM. SUN-1334H free base inhibits histamine-induced bronchoconstriction in guinea pigs, histamine-induced skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guinea pigs.
DC75912 GSK-J1 sodium GSK-J1 sodium is a potent inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A, with IC50 value of 60 nM towards KDM6B.
DC75913 PGD2 ethanolamide PGD2 ethanolamide is the COX-2 dependent metabolite of Anandamide that induces apoptosis in colorectal carcinoma (CRC) cells.
DC75914 Claramine Claramine is a steroid polyamine with blood-brain barrier permeability. Claramine can regulate the properties of lipid membranes and protect cells from various biological toxins, including misfolded protein oligomers and biological protein-based toxins.
DC75915 Empenthrin Empenthrin (S-2852F) is a synthetic pyrethroid. Empenthrin can be used in insecticides. Empenthrin shows a clear species-specificity in the inhibitory effect on the Pentobarbital (PTB)-metabolizing enzyme(s). Empenthrin prolongs PTB induced-sleeping time in mice through an inhibition of the PTB-metabolizing enzyme(s) in the liver, an effect that does not occur in rats. Empenthrin shows a clear species-specificity in the inhibitory effect on the PTB-metabolizing enzyme(s).
DC75916 LH1753 LH1753 is an orally active L-cystine crystallization inhibitor with an EC50 of 29.5 nM. LH1753 can be used for Cystinuria research.
DC75917 Safotibant Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model.
DC75918 Remlarsen sodium Remlarsen (MRG-201), a miR-29b mimic, acts a miR-29b agonist. Remlarsen sodium has the potential for preventiong formation of a fibrotic scar or cutaneous fibrosis.
DC75919 ARC19499 sodium ARC19499 sodium is an aptamer that inhibits tissue factor pathway inhibitor (TFPI) , thereby enabling clot initiation and propagation via the extrinsic pathway. The core aptamer binds tightly and specifically to TFPI. ARC19499 sodium blocks TFPI inhibition of both factor Xa and the TF/factor VIIa complex. ARC19499 sodium corrects thrombin generation in hemophilia A and B plasma and restores clotting in FVIII-neutralized whole blood.

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