BAR501 - GPCR19 Agonist - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBAR501Cat. No.: HY-101274CAS No.: 1632118-69-4分式: CHO分量: 406.64作靶點: GPCR19作通路: GPCR/G Protein儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (122.96 mM)* means soluble, but saturat

2、ion unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.4592 mL 12.2959 mL 24.5918 mL5 mM 0.4918 mL 2.4592 mL 4.9184 mL10 mM 0.2459 mL 1.2296 mL 2.4592 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條

3、件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (6.76 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.75 mg/mL (6.76 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules

4、您邊的抑制劑師www.MedChemESolubility: 2.75 mg/mL (6.76 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 BAR501效選擇性的GPBAR1激動劑，EC50值為1 M。IC50 & Target EC50: 1 M (GPBAR1) 1體外研究 BAR501 is a selective GPBAR1 agonist devoid of FXR agonistic activity. It effectively transactivates GPBAR1in HEK293 cells overexpressing a

5、CRE along with GPBAR1, with an EC50 of 1 M. Exposure of GLUTAgcells to BAR501 (10 M) increases the expression of GLP-1 mRNA by 2.5 folds 1.體內(nèi)研究 Pretreating rats for 6 days with BAR501, 15 mg/kg, reduces basal portal pressure and blunts thevasoconstriction activity of norepinephrine. Pretreatment wit

6、h BAR501 attenuates the hepatic vasomotoractivity induced by shear stress and methoxamine. Administration of BAR501 exerts a direct vasodilatoryactivity in the CCl4 model. Treating mice with BAR501 at the dose of 15 mg/Kg reduces portal pressure andAST plasma levels. BAR501 attenuates endothelial dy

7、sfunction by regulating CSE expression/activity 1.PROTOCOLCell Assay 1 For GPBAR1 mediated transactivation, HEK-293T cells are plated at 10000 cells/well in a 24 well-plate andtransfected with 200 ng of pGL4.29, a reporter vector containing a cAMP response element (CRE) that drivesthe transcription

8、of the luciferase reporter gene luc2P, with 100 ng of pCMVSPORT6-human GPBAR1, andwith 100 ng of pGL4.70. At 24 h post-transfection, HepG2 and HEK293T cells are incubated with 10 MBAR501 for 18 h and luciferase activities are assayed and normalized against the Renilla activities 1.MCE has not indepe

9、ndently confirmed the accuracy of these methods. They are for reference only.Animal Mice: C57BL6 mice are administered i.p. 500 L/Kg body weight of CCl4 in an equal volume of paraffin oilAdministration 1 twice a week for 9 weeks. CCL4 mice are randomized to receive BAR501 (15 mg/Kg daily by gavage)

10、orvehicle (distilled water). Serum bilirubin, albumin, aspartate aminotransferase, alanine aminotransferase andalkaline phosphatase are measured by routine biochemical clinical chemistry 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Renga B, et al. Reversal of Endothelial Dysfunction by GPBAR1 Agonism in Portal Hypertension Involves a AKT/FOXOA1 DependentRegulation of H2S Generation and Endothelin-1. PLoS One. 2015 Nov 5;10(11):e0141082.McePdfHeightCaution: Product has not been