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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

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Purity: 98.79%
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 SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$149-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:98.79%
Color:White to Yellow
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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
PAC1:9200 nM, GLP1 receptor:>10000 nM, VPAC1:>10000 nM, GCGR:6.6 nM (binding), GCGR:15.7 nM (cAMP assay), VPAC2:>10000 nM, GIPR:1020 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].
SynonymsMK0893, 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)
In Vivo Formulation
10% DMSO+90% Corn Oil: 2 mg/mL (3.4 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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