MK 0893

InvivoChem Cat #:V4286CAS #:870823-19-1Purity >=98%

Description: MK-0893 (CRA1; MK0893) is a novel, potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM. MK-0893 is a reversible and competitive antagonist with high binding affinity (IC(50) of 6.6 nM) and functional cAMP activity (IC(50) of 15.7 nM). It is selective for glucagon receptor relative to other family B GPCRs, showing IC(50) values of 1020 nM for GIPR, 9200 nM for PAC1, and > 10000 nM for GLP-1R, VPAC1, and VPAC2. MK-0893 blunted glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys. It also lowered ambient glucose levels in both acute and chronic mouse models: in hGCGR ob/ob mice it reduced 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, compound 9m at 3, and 10 mpk po in feed lowered blood glucose levels by 89% and 94% at day 10, respectively, relative to the difference between the vehicle control and lean hGCGR mice. On the basis of its favorable biological and DMPK properties, MK-0893 was selected for further preclinical and clinical evaluations.

Description:

References: J Med Chem. 2012 Jul 12

References

-20C for 3 years in powder form

Synonym: MK-0893; MK 0893; MK0893; GRA-1; GRA1; GRA 1
IUPAC/Chemical Name: (S)-3-(4-(1-(3-(2-fluoro-5-(trifluoromethyl)phenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl)ethyl)benzamido)propanoic acid
InChi Key: UXPYCHMVTKGDJP-IBGZPJMESA-N
InChi Code: InChI=1S/C33H27F4N3O4/c1-19(20-3-5-21(6-4-20)32(43)38-14-13-31(41)42)40-30(24-8-7-23-16-26(44-2)11-9-22(23)15-24)18-29(39-40)27-17-25(33(35, 36)37)10-12-28(27)34/h3-12, 15-19H, 13-14H2, 1-2H3, (H, 38, 43)(H, 41, 42)/t19-/m0/s1
SMILES Code: O=C(O)CCNC(C1=CC=C([CH](N2N=C(C3=CC(C(F)(F)F)=CC=C3F)C=C2C4=CC=C5C=C(OC)C=CC5=C4)C)C=C1)=O