MK 0893 - 5mg

MK 0893 is a dual inhibitor of the glucagon receptor (GCGR) and insulin-like growth factor 1 receptor (IGF-1R), with IC50 values of 6.6nM and 6nM, respectively [1, 2]. In a receptor-binding assay using CHO cells expressing the human GCGR, MK 0893 effectively inhibits glucagon binding (IC50 of 6.6 ± 3.5nM) and induces cAMP production (IC50 of 15.7 ± 5.4nM). This compound is a competitive, reversible GCGR antagonist, as demonstrated through Schild analysis. It also blunts glucagon-induced glucose excursion in a glucagon challenge model using hGCGR mice, highlighting its potential as an oral treatment for type 2 diabetes. Furthermore, MK 0893 acts as a potent, selective, and orally bioavailable IGF-1R inhibitor, showing strong efficacy in IGF-driven mouse xenograft models.

Chemical Properties:

• Physical Appearance: Solid
• Storage: Store at -20°C
• Molecular Weight: 588.48
• CAS Number: 870823-12-4
• Chemical Formula: C32H27Cl2N3O4
• Synonyms: MK0893, MK-0893
• Solubility: ≥24.05 mg/mL in DMSO; Insoluble in H2O; ≥4.8 mg/mL in EtOH with gentle warming and ultrasonic.
• Chemical Name: (S)-3-(4-(1-(3-(3,5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl)ethyl)benzamido)propanoic acid
• Canonical SMILES: OC(CCNC(C1=CC=C(C@HN2N=C(C3=CC(Cl)=CC(Cl)=C3)C=C2C4=CC=C(C=C(OC)C=C5)C5=C4)C=C1)=O)=O