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首页-小分子抑制剂&激动剂-GPCR-Lysophospholipid Receptor-PIPE-791
PIPE-791

Chemical Structure : PIPE-791

CAS No.: 2901868-37-7

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PIPE-791 (PIPE791)

货号: PC-27238Not For Human Use, Lab Use Only.

PIPE-791 is a potent, selective, oral, brain-penetrant lysophosphatidic acid receptor 1 (LPAR1, LPA1) antagonist with IC50 of 9.9 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

PIPE-791 is a potent, selective, oral, brain-penetrant lysophosphatidic acid receptor 1 (LPAR1, LPA1) antagonist with IC50 of 9.9 nM.
PIPE-791 is more potent than the cis isomer (IC50=112 nM).
PIPE-791 potently binds membranes prepared from cells overexpressing human LPAR1 with Ki of 0.752 nM.
displays functional selectivity (>10-fold) over other LPA receptor isoforms.
PIPE-791 induced OPC differentiation and promoted remyelination following a demyelinating insult in vitro, mitigated the macrophage-mediated inhibition of OPC differentiation and inhibited microglial and fibroblast activation.
PIPE-791 increased oligodendrocyte number, and in the mouse experimental autoimmune encephalomyelitis (EAE) model of MS, promoted myelination, reduced neuroinflammation, and restored visual evoked potential latencies (VEP).

物理化学性质&存储条件

分子量 477.51
分子式 C24H29F2N3O5
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

(1r,4r)-4-(3-(2-(Difluoromethoxy)-6-methoxypyridin-3-yl)-1-(2-isopropylphenyl)ureido)cyclohexane-1-carboxylic acid

参考文献

1. Chen A, et al. J Med Chem. 2026 Jun 29. doi: 10.1021/acs.jmedchem.6c01049.

2. Poon MM, et al. Sci Rep. 2024 May 8;14(1):10573.

3. Hama A, et al. Neuropharmacology. 2025 Dec 1;280:110647.

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