GS-2278 | LPAR1 antagonist | Probechem Biochemicals

Chemical Structure : GS-2278

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GS-2278 (GS2278)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	549.42
分子式	C22H16F5N9O3
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-(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

参考文献

1. Tang DT, et al. J Med Chem. 2024 Nov 21. doi: 10.1021/acs.jmedchem.4c02090.

GS-2278 (GS2278)

生物&药学活性

物理化学性质&存储条件

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GS-2278 (GS2278)

生物&药学活性

物理化学性质&存储条件

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