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首页-小分子抑制剂&激动剂-GPCR-Lysophospholipid Receptor-LPA1 antagonist Compound A
LPA1 antagonist Compound A

Chemical Structure : LPA1 antagonist Compound A

CAS No.: 1614824-42-8

LPA1 antagonist Compound A

货号: PC-24539Not For Human Use, Lab Use Only.

LPA1 antagonist Compound A is a potent, selective, and brain penetrant lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 18.8 nM in 35S-GTPγS binding assays, and IC50 of 12.03 nM in Ca2+ influx assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

LPA1 antagonist Compound A is a potent, selective, and brain penetrant lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 18.8 nM in 35S-GTPγS binding assays, and IC50 of 12.03 nM in Ca2+ influx assays.
Compound A shows IC50 of 27 nM in β-arrestin assay, >25-fold selective over other LPA receptors.
Compound A demonstratesa nti-hyperalgesic effects in the IPGP model mice.

物理化学性质&存储条件

分子量 548.05
分子式 C30H26ClNO5S
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

(R)-1-[4'-(5-chloro-3-{[(1-phenylethoxy)carbonyl] amino}thiophen-2-yl)-2′-methoxy-[1,1′-biphenyl]-4-yl] cyclopropanecarboxylic acid

参考文献

1. Neyama H, et al. J Pharmacol Sci. 2025 Jun;158(2):139-142.

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