| Bioactivity | MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM. | ||||||||||||
| Target | IC50: 6.6 nM (glucagon receptor) | ||||||||||||
| Invitro | MK 0893 is selective for glucagon receptor relative to other family B GPCRs, showing IC50 values of 1020 nM for GIPR, 9200 nM for PAC1, and >10000 nM for GLP-1R, VPAC1, and VPAC2. MK 0893 is active against the rhesus monkey GCGR, showing an IC50 of 56 nM in a cAMP assay with CHO cells expressing the rhesus GCGR[1]. | ||||||||||||
| In Vivo | MK 0893 blunts glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys. It also lowers ambient glucose levels in both acute and chronic mouse models: in hGCGR ob/ob mice it reduces glucose (AUC 0-6 h) by 32% and 39% at 3 and 10 mpk single doses, respectively. In hGCGR mice on a high fat diet, MK 0893 at 3, and 10 mpk po in feed lowers blood glucose levels by 89% and 94% at day 10, respectively, relative to the difference between the vehicle control and lean hGCGR mice[1]. | ||||||||||||
| Name | MK 0893 | ||||||||||||
| CAS | 870823-12-4 | ||||||||||||
| Formula | C32H27Cl2N3O4 | ||||||||||||
| Molar Mass | 588.48 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Xiong Y, et al. Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.J Med Chem. 2012 Jul 12; |