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目录号 : GC13880

agonist of bile acid receptor GPBAR1

GPBAR-A Chemical Structure

Cas No.:877052-79-4

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10mg
¥3,455.00
现货
50mg
¥14,102.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

GPBAR-A is an agonist of bile acid receptor GPBAR1 [1].

The G protein-coupled bile acid receptor 1 (GPBAR1, TGR5) is a plasma membrane-bound receptor for bile acids. TGR5 is involved in gallstone formation and is expressed in the epithelium of human gallbladders [2].

GPBAR-A is an agonist of bile acid receptor GPBAR1. In GLUTag cells, GPBAR-A stimulated glucagon-like peptide (GLP-1) release. In primary colonic cultures, GPBAR-A increased GLP-1 release by 4.2-fold. In upper small intestinal cultures, GPBAR-A increased GLP-1 release by 2.6-fold. In GLUTag cells, GPBAR-A increased cAMP concentration by 57%. Also, GPBAR-A increased calcium in 56/149 cells and caused the mean response by 1.3-fold. In the presence of glucose, GPBAR-A increased calcium in 148/149 cells and caused the mean response by 2.6-fold. In the presence of diazoxide (the KATP channel opener, 340 μM) and 70 mM KCl, GPBAR-A also increased GLP-1 secretion. In colonic and small intestinal cultures, GPBAR-A increased the GLP-1 secretion by 2.4-fold and 1.5-fold. The GLP-1 secretion mediated by GPBAR-A was independent on KATP channel closure [1].

References:
[1].  Parker HE, Wallis K, le Roux CW, et al. Molecular mechanisms underlying bile acid-stimulated glucagon-like peptide-1 secretion. Br J Pharmacol, 2012, 165(2): 414-423.
[2].  Keitel V, Cupisti K, Ullmer C, et al. The membrane-bound bile acid receptor TGR5 is localized in the epithelium of human gallbladders. Hepatology, 2009, 50(3): 861-870.

Chemical Properties

Cas No. 877052-79-4 SDF
分子式 C23H15F7N2O2 分子量 484.37
溶解度 <9.69mg/ml in ethanol; <48.44mg/ml in DMSO 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.0645 mL 10.3227 mL 20.6454 mL
5 mM 0.4129 mL 2.0645 mL 4.1291 mL
10 mM 0.2065 mL 1.0323 mL 2.0645 mL
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