| Identification | Back Directory | [Name]
GPBAR-A | [CAS]
877052-79-4 | [Synonyms]
GPBAR-A
GPBAR-A >=98% (HPLC)
4-[[3,5-Bis(trifluoromethyl)phenyl]methyl]-6-(2-fluorophenyl)-4,5-dihydro-pyrido[3,2-f]-1,4-oxazepin-3(2H)-one
Pyrido[3,2-f]-1,4-oxazepin-3(2H)-one, 4-[[3,5-bis(trifluoromethyl)phenyl]methyl]-6-(2-fluorophenyl)-4,5-dihydro- | [Molecular Formula]
C23H15F7N2O2 | [MOL File]
877052-79-4.mol | [Molecular Weight]
484.37 |
| Chemical Properties | Back Directory | [storage temp. ]
2-8°C | [solubility ]
<9.69mg/ml in ethanol; <48.44mg/ml in DMSO | [form ]
solid | [color ]
Off-white | [InChI]
1S/C23H15F7N2O2/c24-19-4-2-1-3-17(19)16-5-6-31-21-18(16)11-32(20(33)12-34-21)10-13-7-14(22(25,26)27)9-15(8-13)23(28,29)30/h1-9H,10-12H2 | [InChIKey]
ZIXNJVGTAXRKAP-UHFFFAOYSA-N | [SMILES]
O=C(CO1)N(CC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)CC3=C1N=CC=C3C4=C(F)C=CC=C4 |
| Hazard Information | Back Directory | [Uses]
GPBAR-A is a GPBA receptor (TGR5) agonist. | [Biological Activity]
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]. | [storage]
Store at -20°C | [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. |
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| Company Name: |
Energy Chemical
|
| Telephone: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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