Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BAR501 is an effective and specific GPBAR1 agonist (EC50: 1 μM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 57.00 | |
5 mg | In stock | $ 127.00 | |
10 mg | In stock | $ 227.00 | |
25 mg | In stock | $ 383.00 | |
50 mg | In stock | $ 569.00 | |
100 mg | In stock | $ 819.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 113.00 |
Description | BAR501 is an effective and specific GPBAR1 agonist (EC50: 1 μM). |
Targets&IC50 | GPBAR1:1 μM(EC50) |
In vitro | In HEK293 cells overexpressing a CRE along with GPBAR1, BAR501 effectively transactivates GPBAR1 (EC50: 1 μM). In GLUTAg cells, BAR501 (10 μM) increases the mRNA expression of GLP-1 by 2.5 folds. |
In vivo | Pretreating rats for 6 days with BAR501 (15 mg/kg), the basal portal pressure reduces and the vasoconstriction activity of norepinephrine blunts. BAR501 attenuates the hepatic vasomotor activity induced by methoxamine and shear stress. In the CCl4 model, BAR501 exerts a direct vasodilatory activity. BAR501 (15 mg/kg) can reduce AST plasma levels and portal pressure. BAR501 attenuates endothelial dysfunction by regulating CSE expression/activity. |
Cell Research | For GPBAR1 mediated transactivation, HEK-293T cells are plated at 10000 cells/well in a 24 well-plate and transfected with 200 ng of pGL4.29, a reporter vector containing a cAMP response element (CRE) that drives the transcription of the luciferase reporter gene luc2P, with 100 ng of pCMVSPORT6-human GPBAR1, and with 100 ng of pGL4.70. At 24 h post-transfection, HepG2 and HEK293T cells are incubated with 10 μM BAR501 for 18 h and luciferase activities are assayed and normalized against the Renilla activities[1]. |
Animal Research | Animal: C57BL6 miceAdministration: i.p., 500 μL/kg of CCl4 in an equal volume of paraffin oil twice a week for 9 weeks. CCL4 mice are randomized to receive BAR501 (15 mg/Kg daily by gavage) or vehicle (distilled water). Serum bilirubin, albumin, aspartate aminotransferase, alanine aminotransferase and alkaline phosphatase are measured by routine biochemical clinical chemistry[1]. |
Synonyms | BAR 501 |
Molecular Weight | 406.64 |
Formula | C26H46O3 |
CAS No. | 1632118-69-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (122.96 mM)
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
BAR501 1632118-69-4 GPCR/G Protein GPCR19 Inhibitor GPBAR1 BAR-501 TGR5 BAR 501 G-protein coupled receptor 19 G protein-coupled Bile Acid Receptor 1 inhibit inhibitor