| Identification | Back Directory | [Name]
AZD1283 | [CAS]
919351-41-0 | [Synonyms]
AZD1283
CS-1176
AZD1283, >98%
AZD-1283;AZD 1283
AZD1283 , CID23649325
ETHYL 6-(4-{[(BENZYLSULFONYL)AMINO]CARBONYL}PIPERIDIN-1-YL)-5-CYANO-2-METHYLNICOTINATE
6-[4-[[(Benzylsulfonyl)amino]carbonyl]piperidin-1-yl]-5-cyano-2-methylnicotinic acid ethyl ester
Ethyl 5-cyano-2-methyl-6-[4-[[[(phenylmethyl)sulfonyl]amino]carbonyl]-1-piperidinyl]-3-pyridinecarboxylate
ethyl 6-(4-((benzylsulfonyl)carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate AZD1283
3-Pyridinecarboxylic acid, 5-cyano-2-methyl-6-[4-[[[(phenylmethyl)sulfonyl]amino]carbonyl]-1-piperidinyl]-, ethyl ester | [Molecular Formula]
C23H26N4O5S | [MDL Number]
MFCD26395344 | [MOL File]
919351-41-0.mol | [Molecular Weight]
470.54 |
| Hazard Information | Back Directory | [Uses]
AZD 1283 is a non-nucleotide reversible antagonist of P2Y12R, which regulates platelet activation and thrombus formation. | [Biological Activity]
the central role of the p2y12 receptor in platelet function makes it an attractive target for the development of novel antiplatelet therapies. azd1283 is found to be a potent, selective and reversible antagonist of the p2y12 receptor. | [in vitro]
it was observed that the benzylic azd1283 and its analogue 13 were both potent in the higher order residual platelet count assay in which the two tested 5-chlorothienyls showed low (ic50 >22 μm) potency [1]. | [in vivo]
in a modified folts model in dog, both azd1283 and its analogue 13 could dose-dependently induce increases in blood flow and inhibition of adp-induced platelet aggregation with antithrombotic ed50 values of 3.0 and 10.0 μg/kg/min, respectively. the dose that induced a larger than 3-fold increase in bleeding time were 33 and 100 μg/kg/min for azd1283 and 13, respectively [2]. | [IC 50]
0.011, 0.025 and 3.2 μm for binding, gtpγs and residual platelet count (rpc), respectively | [storage]
Store at -20°C | [References]
[1] bach p, antonsson t, bylund r, bj?rkman ja, ?sterlund k, giordanetto f, van giezen jj, andersen sm, zachrisson h, zetterberg f. 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;56(17):7015-24. |
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| Company Name: |
SPIRO PHARMA
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| Tel: |
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| Website: |
www.spiropharma.com.cn |
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