BAR 501

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BAR501 是一种有效且特异性的 GPBAR1 激动剂 (EC50: 1 μM)。

BAR-501 is a selective GPBAR1 agonist devoid of any FXR agonistic activity. BAR501 effectively reduced hepatic perfusion pressure and counteracted the vasoconstriction activity of norepinephrine. BAR501 rescues from endothelial dysfunction in rodent models of portal hypertension by exerting genomic and non-genomic effects on CSE, eNOS and ET-1 in liver sinusoidal cells.

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 μM. Exposure of GLUTAg cells to BAR501 (10 μM) increases the expression of GLP-1 mRNA by 2.5 folds.

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.

BAR-501 | BAR 501 | BAR501

Membrane Transporter/Ion Channel

Monocarboxylate Transporter

GPBAR1

Endocrinology

——

1632118-69-4

406.65

C26H46O3

>98% (HPLC)

DMSO : ≥ 50 mg/mL. 122.96 mM

CC[C@H]1[C@@H]2C[C@@H](CC[C@@]2([C@H]2CC[C@]3([C@H]([C@@H]2[C@H]1O)CC[C@@H]3[C@H](C)CCCO)C)C)O

(3R,5S,6S,7S,8S,9S,10S,13R,14S,17R)-6-ethyl-17-((R)-5-hydroxypentan-2-yl)-10,13-dimethylhexadecahydro-1H-cyclopenta[a]phenanthrene-3,7-diol

(-20℃)

With Ice Pack

≥ 2 years