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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-5-HT2A antagonist 11c
5-HT2A antagonist 11c

Chemical Structure : 5-HT2A antagonist 11c

CAS No.: 2641482-08-6

5-HT2A antagonist 11c

货号: PC-21787Not For Human Use, Lab Use Only.

5-HT2A antagonist 11c is a potent, selective, peripheral 5HT2A antagonist with IC50 of 14 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

5-HT2A antagonist 11c is a potent, selective, peripheral 5HT2A antagonist with IC50 of 14 nM.
5-HT2A antagonist 11c shows good chemical, hepatocyte, and plasma stability, no significant cytotoxicity in five representative mammalian cell lines (VERO, HFL-1, L929, NIH3T3, CHO-K1).
5-HT2A antagonist 11c shows selective inhibition of 5HT2A among other 5-HT subtypes.
5-HT2A antagonist 11c (5 and 10 mpk) daily oral gavage attenuates HFD-induced obesity, MASLD, and metabolic syndrome.
5-HT2A antagonist 11c shows vivo efficacy against CDAHFD-induced liver fibrosis and inflammation C57BL/6 J mice.
5-HT2A antagonist 11c is a novel peripheral 5HT2A antagonist for Metabolic Dysfunction-Associated Steatohepatitis (MASH) and steatosis under clinical investigations.

物理化学性质&存储条件

分子量 517.07
分子式 C30H33ClN4O2
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

3-(2-(4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidin-1-yl)ethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one

参考文献

1. Haushabhau S Pagire, et al. Nat Commun. 2024 Jan 20;15(1):645.

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