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首页-小分子抑制剂&激动剂-GPCR-Endothelin Receptor-Aprocitentan
Aprocitentan

Chemical Structure : Aprocitentan

CAS No.: 1103522-45-7

Aprocitentan (ACT-132577, ACT132577)

货号: PC-60030Not For Human Use, Lab Use Only.

Aprocitentan (ACT132577) is the major and pharmacologically active metabolite of Macitentan, an orally active, dual endothelin receptor antagonist with IC50s of 3.4 nM and 987 nM for ETA/ETB receptor respectively, inhibits ET-1 and ET-2-induced contractions in functional assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Aprocitentan (ACT132577) is the major and pharmacologically active metabolite of Macitentan, an orally active, dual endothelin receptor antagonist with IC50s of 3.4 nM and 987 nM for ETA/ETB receptor respectively, inhibits ET-1 and ET-2-induced contractions in functional assays.

物理化学性质&存储条件

分子量 546.194
分子式 C16H14Br2N6O4S
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

N-[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]sulfuric diamide

参考文献

1. Iglarz M, et al. J Pharmacol Exp Ther. 2008 Dec;327(3):736-45.

2. Kummer O, et al. Eur J Pharm Sci. 2009 Nov 5;38(4):384-8.

3. Sidharta PN, et al. Eur J Clin Pharmacol. 2011 Oct;67(10):977-84.

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