Chemical Structure : MK-0893
CAS No.: 870823-12-4
Catalog No.: PC-45831Not For Human Use, Lab Use Only.
A potent, selective, reversible and competitive antagonist of glucagon receptor with high binding affinity (IC(=50=6.6 nM) and functional cAMP activity (IC50=15.7 nM).
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MK-0893 is a potent, selective, reversible and competitive antagonist of glucagon receptor with high binding affinity (IC(=50=6.6 nM) and functional cAMP activity (IC50=15.7 nM).
MK-0893 displays selectivity for glucagon receptor relative to other family B GPCRs, IC50 of 1020 nM for GIPR, 9200 nM for PAC1, and >10000 nM for GLP-1R, VPAC1, and VPAC2.
MK-0893 blunts glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys, also lowers ambient glucose levels in both acute and chronic mouse models.
M.Wt | 588.4805 | |
Formula | C32H27Cl2N3O4 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
.beta.-Alanine, N-[4-[(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methoxy-2-naphthalenyl)-1H-pyrazol-1-yl]ethyl]benzoyl]- |
1. Xiong Y, et al. J Med Chem. 2012 Jul 12;55(13):6137-48.
2. Guan HP, et al. J Lipid Res. 2015 Nov;56(11):2183-95.
3. Jazayeri A, et al. Nature. 2016 May 12;533(7602):274-7.
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