191034-25-0 Usage
Uses
L- is a potent (Kb = 25 nM), selective antagonist of glucagon.
Biological Activity
Very potent and selective, non-competitive antagonist of the human glucagon receptor (hGR). Binds with high affinity to human GR (IC 50 = 3.7 nM), and moderate affinity to murine and canine GRs (IC 50 values are 63 and 60 nM respectively). In contrast, displays poor affinity for rat, guinea pig, and rabbit glucagon receptors (IC 50 > 1 μ M). In functional studies, inhibits glucagon-stimulated cAMP synthesis in CHO cells expressing hGR (IC 50 = 41 nM), and in murine liver membranes. Orally active in vivo .
Check Digit Verification of cas no
The CAS Registry Mumber 191034-25-0 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,9,1,0,3 and 4 respectively; the second part has 2 digits, 2 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 191034-25:
(8*1)+(7*9)+(6*1)+(5*0)+(4*3)+(3*4)+(2*2)+(1*5)=110
110 % 10 = 0
So 191034-25-0 is a valid CAS Registry Number.
InChI:InChI=1/C24H20BrClN2O/c1-2-13-29-23-8-5-18(25)14-20(23)21-15-22(16-3-6-19(26)7-4-16)28-24(21)17-9-11-27-12-10-17/h3-12,14-15,28H,2,13H2,1H3
191034-25-0Relevant articles and documents
Potent, orally absorbed glucagon receptor antagonists
De Laszlo, Stephen E.,Hacker, Candice,Li, Bing,Kim, Dooseop,MacCoss, Malcolm,Mantlo, Nathan,Pivnichny, James V.,Colwell, Larry,Koch, Gregory E.,Cascieri, Margaret A.,Hagmann, William K.
, p. 641 - 646 (2007/10/03)
The SAR of 2-pyridyl-3,5-diaryl pyrroles, ligands of the human glucagon receptor and inhibitors of p38 kinase, were investigated. This effort resulted in the identification of 2-(4-pyridyl)-5-(4-chlorophenyl)-3-(5- bromo-2-propyloxyphenyl)pyrrole 49 (L-168,049), a potent (Kb = 25 nM), selective antagonist of glucagon.
