AZD1283

An antagonist of the P2Y12 receptor

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5mg

￥1262.00

1010.00

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10mg

￥2200.00

1760.00

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50mg

￥5375.00

4300.00

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100mg

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货号: ajci14154
CAS: 919351-41-0
别名: AZD 1283, 6-4-(Benzylsulfonyl)aminocarbonylpiperidin-1-yl-5-cyano-2-methylnicotinic acid ethyl ester
分子式: C23H26N4O5S
分子量: 470.54
纯度: >98%
溶解度: ≥ 18.15mg/mL in DMSO
储存: Store at -20°C
库存: 现货

Background

IC50: 0.011, 0.025 and 3.2 μM for binding, GTPγS and residual platelet count (RPC), respectively

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].

Clinical trials: Currenlty there is no clinical data available.

Reference:
[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.

Protocol

Animal experiment [1]:
Animal models	A modified Folts dog model
Dosage form	0.1 ~ 33 μg/(kg × min); 5 consecutive 30 min periods
Applications	AZD1283 dose-dependently increased blood flow and inhibited ADP-induced platelet aggregation with an antithrombotic ED50 value of 3 μg/(kg × min). A dose higher than 33 μg/(kg × min) was required for induction of a larger than 3.5-fold increase in bleeding time.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
参考文献: [1]. Bach P, Antonsson T, Bylund R, Bjrkman 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.