Chemical Structure : GS-2278
CAS No.:
2750508-72-4
GS-2278
(GS2278)
Catalog No.: PC-23559Not For Human Use, Lab Use Only.
GS-2278 is a potent, selective lysophosphatidic acid receptor 1 (LPAR1, LPA1) antagonist with EC50 of 12 nM in MRTF-A nuclear translocation assay in TWNT4 cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
GS-2278 is a potent, selective lysophosphatidic acid receptor 1 (LPAR1, LPA1) antagonist with EC50 of 12 nM in MRTF-A nuclear translocation assay in TWNT4 cells.
GS-2278 shows high selectivity for LPAR1 over LPAR2, LPAR3, and LPAR5 in the calcium (Ca2+) assays performed in CHO cell lines overexpressing the individual receptors.
GS-2278 antagonized all LPAR1 downstream pathways (Gαi, Gα12/13, Gαq, β-Arrestin) indicating unbiased antagonism.
GS-2278 binding to LPAR1 is competitive with LPA, with a Ki of 60 nM for human LPAR1 in a [3H]-LPA binding assay.
GS-2278 dose-dependently blocked LPA-induced histamine release and demonstrated efficacy in an interventional model of bleomycin-induced lung fibrosis.
Physicochemical Properties
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M.Wt
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549.42
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Formula
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C22H16F5N9O3
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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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(R)-1-(2,5-Difluoropyridin-3-yl)ethyl (1-Methyl-4-(5-(2-(trifluoromethyl)pyrimidine-5-carboxamido)pyridin-2-yl)-1H-1,2,3-triazol-5-yl)carbamate
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References
1. Tang DT, et al. J Med Chem. 2024 Nov 21. doi: 10.1021/acs.jmedchem.4c02090.
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