化合物BAR 501 T4083
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
1 mg | 1632118-69-4 | ¥496.00 | 询底价 |
5 mg | 1632118-69-4 | ¥1,080.00 | 询底价 |
50 mg | 1632118-69-4 | ¥5,170.00 | 询底价 |
1 mL | 1632118-69-4 | ¥997.00 | 询底价 |
10 mg | 1632118-69-4 | ¥1,830.00 | 询底价 |
100 mg | 1632118-69-4 | ¥7,320.00 | 询底价 |
25 mg | 1632118-69-4 | ¥3,580.00 | 询底价 |
Product Introduction
Bioactivity
英文名: BAR501
描述: BAR501是高效选择性的 GPBAR1激动剂(EC50:1 μM)。
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].
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.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 50 mg/mL (122.96 mM)
关键字: Inhibitor | GPBAR1 | BAR-501 | TGR5 | GPCR19 | G-protein coupled receptor 19 | G protein-coupled Bile Acid Receptor 1 | BAR501 | inhibit
相关产品: INT-777 | PEN (human) aceate | Ursodeoxycholic acid sodium | INT-767 | SBI-115 | Deoxycholic acid | L-692429 | SB756050 | Deoxycholic acid sodium salt | TC-G 1005
相关库: Anti-COVID-19 Compound Library | Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | NO PAINS Compound Library | Anti-Infection Compound Library | Bioactive Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途