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.
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.
