- Potent, orally absorbed glucagon receptor antagonists
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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.
- 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.
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p. 641 - 646
(2007/10/03)
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