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BAR501是高效选择性的 GPBAR1激动剂(EC50:1 μM)。
BAR501是高效选择性的 GPBAR1激动剂(EC50:1 μM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 496 | 现货 | |
5 mg | ¥ 1,080 | 现货 | |
10 mg | ¥ 1,830 | 现货 | |
25 mg | ¥ 3,580 | 现货 |
产品描述 | BAR501 is an effective and specific GPBAR1 agonist (EC50: 1 μM). |
靶点活性 | GPBAR1:1 μM(EC50) |
体外活性 | 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. |
体内活性 | 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. |
细胞实验 | 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]. |
动物实验 | 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]. |
别名 | BAR 501 |
分子量 | 406.64 |
分子式 | C26H46O3 |
CAS No. | 1632118-69-4 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 50 mg/mL (122.96 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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