1197300-24-5 Usage
Description
TGR5 receptor agonist is an agonist of the bile acid G protein-coupled receptor TGR5 (EC50s = 31.6-158.5 nM in cell-based assays). It stimulates cAMP formation in HEK293 cells expressing TGR5 (EC50 = 2.3 pM). TGR5 receptor agonist (1 mg/kg) increases glucagon-like peptide 1 (GLP-1) secretion and decreases glucose levels in the hepatic portal vein in dogs when administered in combination with glucose. It also inhibits the cytochrome P450 (CYP) isozymes CYP2C19 and CYP3A4 (IC50s = 316.2 and 1,259 nM, respectively).
Check Digit Verification of cas no
The CAS Registry Mumber 1197300-24-5 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,9,7,3,0 and 0 respectively; the second part has 2 digits, 2 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 1197300-24:
(9*1)+(8*1)+(7*9)+(6*7)+(5*3)+(4*0)+(3*0)+(2*2)+(1*4)=145
145 % 10 = 5
So 1197300-24-5 is a valid CAS Registry Number.
1197300-24-5Relevant articles and documents
Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists
Evans, Karen A.,Budzik, Brian W.,Ross, Sean A.,Wisnoski, David D.,Jin, Jian,Rivero, Ralph A.,Vimal, Mythily,Szewczyk, George R.,Jayawickreme, Channa,Moncol, David L.,Rimele, Thomas J.,Armour, Susan L.,Weaver, Susan P.,Griffin, Robert J.,Tadepalli, Sarva M.,Jeune, Michael R.,Shearer, Todd W.,Chen, Zibin B.,Chen, Lihong,Anderson, Donald L.,Becherer, J. David,De Los Frailes, Maite,Colilla, Francisco Javier
supporting information; experimental part, p. 7962 - 7965 (2010/07/13)
A series of 3-aryl-4-isoxazolecarboxamides identified from a high-throughput screening campaign as novel, potent small molecule agonists of the human TGR5 G-protein coupled receptor is described. Subsequent optimization resulted in the rapid identificatio
