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MK 0893

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Catalog No. T12055Cas No. 870823-12-4
Alias MK0893, L-001241689, L001241689

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.

MK 0893

MK 0893

😃Good
Catalog No. T12055Alias MK0893, L-001241689, L001241689Cas No. 870823-12-4
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 SizePriceAvailabilityQuantity
25 mg$1,8708-10 weeks
50 mg$2,7688-10 weeks
100 mg$4,9508-10 weeks
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Product Introduction

Bioactivity
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].
AliasMK0893, L-001241689, L001241689
Chemical Properties
Molecular Weight588.48
FormulaC32H27Cl2N3O4
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 & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM1.6993 mL8.4965 mL16.9929 mL84.9647 mL
5 mM0.3399 mL1.6993 mL3.3986 mL16.9929 mL
10 mM0.1699 mL0.8496 mL1.6993 mL8.4965 mL
20 mM0.0850 mL0.4248 mL0.8496 mL4.2482 mL
50 mM0.0340 mL0.1699 mL0.3399 mL1.6993 mL

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