919351-41-0

919351-41-0 structure

Name: AZD 1283
Chemical Name: 3-Pyridinecarboxylic acid, 5-cyano-2-methyl-6-[4-[[[(phenylmethyl)sulfonyl]amino]carbonyl]-1-piperidinyl]-, ethyl ester
CAS Number: 919351-41-0
Molecular Formula: C₂₃H₂₆N₄O₅S
Molecular Weight: 470.541
Catalog: Signaling Pathways GPCR/G Protein P2Y Receptor
Create Date: 2016-04-22 00:10:54
Modify Date: 2024-01-09 17:27:26
AZD1283 is a potent antagonist of the P2Y12 receptor with EC50 of 3.0 ug/kg/min, TI >10; with binding IC50 of 11 nM.IC50 value: 3.0 ug/kg/min(EC50) [1]Target: P2Y12 receptor inhibitorAZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses that induced a larger than 3-foldincrease in bleeding time were 33 and 100 μg/kg/min for 3 and 13, respectively. Thus, the therapeutic index (TI) was ≥10 forboth compounds. On the basis of these data, compound 3 was progressed into human clinical trials as candidate drug AZD1283.

Name	3-Pyridinecarboxylic acid, 5-cyano-2-methyl-6-[4-[[[(phenylmethyl)sulfonyl]amino]carbonyl]-1-piperidinyl]-, ethyl ester
Synonyms	AZD 1283 Ethyl 6-{4-[(benzylsulfonyl)carbamoyl]-1-piperidinyl}-5-cyano-2-methylnicotinate 3-Pyridinecarboxylic acid, 5-cyano-2-methyl-6-[4-[[[(phenylmethyl)sulfonyl]amino]carbonyl]-1-piperidinyl]-, ethyl ester 6-[4-[[(Benzylsulfonyl)amino]carbonyl]piperidin-1-yl]-5-cyano-2-methylnicotinic acid ethyl ester AZD1283

Description	AZD1283 is a potent antagonist of the P2Y12 receptor with EC50 of 3.0 ug/kg/min, TI >10; with binding IC50 of 11 nM.IC50 value: 3.0 ug/kg/min(EC50) [1]Target: P2Y12 receptor inhibitorAZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 and 10 μg/kg/min, respectively. The doses that induced a larger than 3-foldincrease in bleeding time were 33 and 100 μg/kg/min for 3 and 13, respectively. Thus, the therapeutic index (TI) was ≥10 forboth compounds. On the basis of these data, compound 3 was progressed into human clinical trials as candidate drug AZD1283.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> P2Y Receptor Research Areas >> Cardiovascular Disease
References	[1]. Bach P, et al. Lead optimization of ethyl 6-aminonicotinate acyl sulfonamides as antagonists of the P2Y12 receptor. separation of the antithrombotic effect and bleeding for candidate drug AZD1283. J Med Chem. 2013 Sep 12;56(17):7015-24.