Chemical Structure : PIPE-791
CAS No.:
2901868-37-7
PIPE-791
(PIPE791)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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).
Physicochemical Properties
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M.Wt
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477.51
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Formula
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C24H29F2N3O5
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(1r,4r)-4-(3-(2-(Difluoromethoxy)-6-methoxypyridin-3-yl)-1-(2-isopropylphenyl)ureido)cyclohexane-1-carboxylic acid
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References
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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