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首页-小分子抑制剂&激动剂-GPCR-P2Y Receptor-ACT-246475
ACT-246475

Chemical Structure : ACT-246475

CAS No.: 1159500-34-1

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ACT-246475 (Selatogrel, ACT246475, ACT 246475)

货号: PC-35577Not For Human Use, Lab Use Only.

Selatogrel (ACT-246475) is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM.

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5 mg ￥2480 In stock
10 mg ￥3980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Selatogrel (ACT-246475) is a potent, selective, reversible P2Y12 receptor antagonist with binding IC50 of 1.0 nM.
ACT-246475 displays no agonist binding activity against P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, and P2Y13 at 10 uM, to P2Y1, P2Y2, P2Y4, P2Y6, P2Y11, no antagonistic activity on P2X1, P2X2, P2X3, P2X4, and P2X7 receptors, as well as a broad panel of receptors, transporters, and enzymes.
ACT-246475 inhibits plateletaggregation with IC50 of 8.0 nM in the light transmission aggregometry (LTA) assay.
ACT-246475 showes efficacy in the rat ferric chloride thrombosis model when administered intravenously.

物理化学性质&存储条件

分子量 618.628
分子式 C28H39N6O8P
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-((R)-2-{[6-((S)-3-Methoxypyrrolidin-1-yl)-2-phenylpyrimidine-4-carbonyl]amino}-3-phosphonopropionyl)piperazine-1-carboxylic acid butyl ester

参考文献

1. Caroff E, et al. J Med Chem. 2015 Dec 10;58(23):9133-53.

2. Rey M, et al. Pharmacol Res Perspect. 2017 Oct;5(5).

3. Juif PE, et al. J Clin Pharmacol. 2018 Aug 8. doi: 10.1002/jcph.1296.

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