BAR501

1632118-69-4

C26H46O3

DMSO : >= 50 mg/mL (122.96 mM)

GPCR/G Protein

BAR501 is a potent and selective agonist of GPBAR1 with an EC₅₀ of 1 uM. IC50 & Target: EC50: 1 uM (GPBAR1)^[1] In Vitro: BAR501 is a selective GPBAR1 agonist devoid of FXR agonistic activity. It effectively transactivates GPBAR1 in HEK293 cells overexpressing a CRE along with GPBAR1, with an EC₅₀ of 1 uM. Exposure of GLUTAg cells to BAR501 (10 uM) increases the expression of GLP-1 mRNA by 2.5 folds^[1]. In Vivo: Pretreating rats for 6 days with BAR501, 15 mg/kg, reduces basal portal pressure and blunts the vasoconstriction activity of norepinephrine. Pretreatment with BAR501 attenuates the hepatic vasomotor activity induced by shear stress and methoxamine. Administration of BAR501 exerts a direct vasodilatory activity in the CCl4 model. Treating mice with BAR501 at the dose of 15 mg/Kg reduces portal pressure and AST plasma levels. BAR501 attenuates endothelial dysfunction by regulating CSE expression/activity^[1].