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MK-0893

Chemical Structure : MK-0893

CAS No.: 870823-12-4

MK-0893 (MK0893;MK 0893)

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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Biological Activity

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.

Physicochemical Properties

M.Wt 588.4805
Formula C32H27Cl2N3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

.beta.-Alanine, N-[4-[(1S)-1-[3-(3,5-dichlorophenyl)-5-(6-methoxy-2-naphthalenyl)-1H-pyrazol-1-yl]ethyl]benzoyl]-

References

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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