2,2-二甲基丙酸3-(2-氯-6-甲基氨基嘌呤-9-基)-2-(2,2-二甲基-丙酰氧基甲基)-丙酯

用途

MRS2395是双雪腐镰刀菌酰基衍生物,是一种有效的P2Y12受体拮抗剂。MRS2395以3.6μM的Ki抑制ADP诱导的血小板活化。MRS2395以7μM的IC50抑制PGE1存在时大鼠血小板中ADP诱导的cAMP。MRS2395增强血小板致密颗粒释放以响应TRAP-6[1][2]。

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名称

[ CAS 号 ]:
491611-55-3

[ 中文名 ]:
2,2-二甲基丙酸3-(2-氯-6-甲基氨基嘌呤-9-基)-2-(2,2-二甲基-丙酰氧基甲基)-丙酯

[ 英文名 ]:
MRS 2395

[英文别名 ]:

mrs 2395

生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> P2Y受体

[参考文献]

[1]. Bin Xu, et al.Acyclic analogues of adenosine bisphosphates as P2Y receptor antagonists: phosphate substitution leads to multiple pathways of inhibition of platelet aggregation. J Med Chem. 2002 Dec 19;45(26):5694-709.

[2]. Annachiara Mitrugno, et al. Potentiation of TRAP-6-induced platelet dense granule release by blockade of P2Y 12 signaling with MRS2395. Platelets. 2018 Jun;29(4):383-394.

物理化学性质

[ 分子式 ]:
C₂₀H₃₀ClN₅O₄

[ 分子量 ]:
439.93600

[ 精确质量 ]:
439.19900

[ PSA ]:
108.23000

[ LogP ]:
3.38920

[ 外观性状 ]:
固体

[ 储存条件 ]:
室温

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

文献

Acyclic analogues of adenosine bisphosphates as P2Y receptor antagonists: phosphate substitution leads to multiple pathways of inhibition of platelet aggregation.

J. Med. Chem. 45 , 5694-5709, (2002)

Activation by ADP of both P2Y(1) and P2Y(12) receptors in platelets contributes to platelet aggregation, and antagonists at these receptor subtypes have antithrombotic properties. In an earlier public...

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