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Beschreibung

A cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GPR40 (EC50 ~50 nM) with much reduced activity towards family members GPR120 (EC50 ~3.5 µ,M), GPR41/GPR43 (EC50 >50 µ,M), as well as a panel of eight other fatty acid and prostaglandin receptors. Shown to induces GPR40-dependent Ca2+ mobilization in HEK-293 cells and potentiate glucose-stimulated insulin secretion in MIN6 cells. Reported to exhibit an in vivo half-life of >=5.3 hr. in rat (p.o. or i.v.) with a bioavailability of 65% and a clearance of 24.9 ml/min/kg., A cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40 (EC50 ~50 nM) with much reduced activity towards family members GRP120 (EC50 ~3.5 µ,M), GRP41/GRP43 (EC50 >50 µ,M), as well as a panel of eight other fatty acid and prostaglandin receptors. Shown to induces GPR40-dependent Ca2+ mobilization in HEK-293 cells and potentiate glucose-stimulated insulin secretion in MIN6 cells. Reported to exhibit an in vivo half-life of >=5.3 hr. in rat (p.o. or i.v.) with a bioavailability of 65% and a clearance of 24.9 ml/min/kg.