AZD 1283

Names

[ CAS No. ]:
919351-41-0

[ Name ]:
AZD 1283

[Synonym ]:
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

Biological Activity

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C₂₃H₂₆N₄O₅S

[ Molecular Weight ]:
470.541

[ Exact Mass ]:
470.162384

[ PSA ]:
137.84000

[ LogP ]:
2.66

[ Appearance of Characters ]:
white solid

[ Index of Refraction ]:
1.618

[ Storage condition ]:
-20℃

AZD 1283

Names

Biological Activity

Chemical & Physical Properties

Related Compounds