Shopping Cart
- Remove All
- Your shopping cart is currently empty
MK 0893 is a potent and selective Glucagon Receptor (GR) antagonist (IC50=6.6 nM) with competitive, reversible, high binding affinity and functional cAMP activity, which attenuates glucagon induced blood glucose elevation and reduces ambient glucose levels in acute and chronic mouse models.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $1,870 | 8-10 weeks | |
50 mg | $2,768 | 8-10 weeks | |
100 mg | $4,950 | 8-10 weeks |
Description | MK 0893 is a potent and selective Glucagon Receptor (GR) antagonist (IC50=6.6 nM) with competitive, reversible, high binding affinity and functional cAMP activity, which attenuates glucagon induced blood glucose elevation and reduces ambient glucose levels in acute and chronic mouse models. |
Targets&IC50 | VPAC2:>10000 nM, GCGR:15.7 nM (cAMP assay), GLP1R:>10000 nM, GIPR:1020 nM, PAC1:9200 nM, GCGR:6.6 nM (binding), VPAC1:>10000 nM |
In vitro | MK 0893 is a potent, reversible, and competitive antagonist of the glucagon receptor (GCGR), exhibiting high binding affinity (IC₅₀ = 6.6 nM) and inhibitory activity in a cAMP functional assay (IC₅₀ = 15.7 nM). MK 0893 is highly selective for GCGR over other class B GPCRs, with IC₅₀ values of 1020 nM for GIPR, 9200 nM for PAC1, and >10000 nM for GLP-1R, VPAC1, and VPAC2[1]. |
In vivo | In hGCGR transgenic mice and rhesus monkeys, MK 0893 effectively blunted glucagon-induced blood glucose elevation. In hGCGR ob/ob mice, single oral doses of 3 and 10 mg/kg reduced glucose AUC (0–6 h) by 32% and 39%, respectively. In hGCGR mice on a high-fat diet, daily feeding of 3 and 10 mg/kg for 10 days reduced blood glucose levels by 89% and 94%, respectively, relative to the difference between vehicle-treated and lean control mice[1]. |
Alias | MK0893, L-001241689, L001241689 |
Molecular Weight | 588.48 |
Formula | C32H27Cl2N3O4 |
Cas No. | 870823-12-4 |
Smiles | [C@@H](C)(N1C(=CC(=N1)C2=CC(Cl)=CC(Cl)=C2)C3=CC4=C(C=C3)C=C(OC)C=C4)C5=CC=C(C(NCCC(O)=O)=O)C=C5 |
Relative Density. | 1.33 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 30 mg/mL (50.98 mM), Sonication is recommended. H2O: < 0.1 mg/mL (insoluble) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
|
Copyright © 2015-2025 TargetMol Chemicals Inc. All Rights Reserved.