AZD1283

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AZD1283 是一种有效的 P2Y12 受体拮抗剂（EC50：3.0 ug/kg/min，结合 IC50：11 nM）。

AZD1283 is a potent antagonist of the P2Y12 receptor. In a modified Folts model in dog, both AZD1283 dose-dependently induced increases in blood flow and inhibition of ADP-induced platelet aggregation with antithrombotic ED50 values of 3.0 μg/kg/min. The doses that induced a larger than 3-fold increase in bleeding time were 33 μg/kg/min. Thus, the therapeutic index (TI) was ≥ 10. On the basis of these data, AZD1283 was progressed into human clinical trials as candidate drug.

AZD1283 exhibits excellent antiplatelet aggregation potency with an IC50 value of 3.6 μM.AZD1283 has highly inhibitory activity against CYP450 with IC50 values of 6.62 μM, 0.399 μM and 4.28 μM and 3.64 μM for CYP2C9, CYP2C19, CYP3A4 (Midazolam as the substrate) and CYP3A4 (Testosterone as the substrate), respectively.AZD1283 induces increases in blood flow and inhibition of ADP-induced platelet aggregation with an antithrombotic EC50 value of 3 μg/(kg×min).

AZD1283 exhibits poor liver microsomal stability in rat (T1/2 = 6.08 min), but better in dog microsomes (T1/2 = 201 min) and human microsomes (T1/2 = 65.0 min). Animal Model:Sprague-Dawley rats Dosage:5 mg/kg Administration:p.o.; single dosage Result:Exhibited a Cmax of 25.9 ± 11 ng/mL, a T1/2 of 1.68 ± 0.37 h and a Tmax of 0.25 h.

AZD-1283 | AZD1283 | AZD 1283

Angiogenesis

PDE

P2Y12

Cardiovascular Disease

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919351-41-0

470.54

C23H26N4O5S

>98% (HPLC)

DMSO : 100 mg/mL. 212.52 mM;H2O : < 0.1 mg/mL

CCOC(=O)c1c(nc(c(c1)C#N)N1CCC(CC1)C(=O)NS(=O)(=O)Cc1ccccc1)C

ethyl 6-(4-((benzylsulfonyl)carbamoyl)piperidin-1-yl)-5-cyano-2-methylnicotinate.

(-20℃)

With Ice Pack

≥ 2 years