AZD 1283

Modify Date: 2024-01-09 17:27:26

AZD 1283 Structure
AZD 1283 structure
Common Name AZD 1283
CAS Number 919351-41-0 Molecular Weight 470.541
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C23H26N4O5S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of AZD 1283


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.

 Names

Name 3-Pyridinecarboxylic acid, 5-cyano-2-methyl-6-[4-[[[(phenylmethyl)sulfonyl]amino]carbonyl]-1-piperidinyl]-, ethyl ester
Synonym More Synonyms

 AZD 1283 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
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.

 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℃

 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
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