1. GPCR/G Protein
  2. Glucagon Receptor

MK 0893 (Synonyms: MK0893; MK-0893)

Cat. No.: HY-50663 Purity: 99.22%
Data Sheet SDS Handling Instructions

MK 0893 is a potent, selective glucagon receptor antagonist with IC50 of 6.6 nM, and > 200 fold selectivity against GIPR, PAC1, GLP-1R, VPAC1 and VPAC2.

For research use only. We do not sell to patients.
MK 0893 Chemical Structure

MK 0893 Chemical Structure

CAS No. : 870823-12-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 489 In-stock
5 mg USD 378 In-stock
10 mg USD 684 In-stock
50 mg USD 1710 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

MK 0893 is a potent, selective glucagon receptor antagonist with IC50 of 6.6 nM, and > 200 fold selectivity against GIPR, PAC1, GLP-1R, VPAC1 and VPAC2.

IC50 & Target

IC50: 6.6 nM (glucagon receptor)

In Vitro

MK 0893 is selective for glucagon receptor relative to other family B GPCRs, showing IC50 values of 1020 nM for GIPR, 9200 nM for PAC1, and >10000 nM for GLP-1R, VPAC1, and VPAC2. MK 0893 is active against the rhesus monkey GCGR, showing an IC50 of 56 nM in a cAMP assay with CHO cells expressing the rhesus GCGR[1].

In Vivo

MK 0893 blunts glucagon-induced glucose elevation in hGCGR mice and rhesus monkeys. It also lowers ambient glucose levels in both acute and chronic mouse models: in hGCGR ob/ob mice it reduces 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, MK 0893 at 3, and 10 mpk po in feed lowers blood glucose levels by 89% and 94% at day 10, respectively, relative to the difference between the vehicle control and lean hGCGR mice[1].

Clinical Trial
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References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.6993 mL 8.4965 mL 16.9929 mL
5 mM 0.3399 mL 1.6993 mL 3.3986 mL
10 mM 0.1699 mL 0.8496 mL 1.6993 mL
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

MK 0893 is diluted from DMSO stocks and added to the assay at a final concentration of 5% DMSO.

CHO hGCGR cells are grown in Iscove's Modified Dulbecco’s Medium (IMDM), 10% FBS, 1 mM l-glutamine, penicillin-streptomycin (100 μ/mL), and 500μg G418/mL for 3-4 days before harvesting using Enzyme-Free Dissociation Media (EFDM). The cells are centrifuged at low speed and resuspended in stimulation buffer. Compounds are diluted from DMSO stocks and added to the assay at a final concentration of 5% DMSO. Cells are preincubated with compound or DMSO controls for 30 min. Glucagon (250 pM) is added, and the samples are incubated at room temperature for an additional 30 min. The assay is terminated with the addition of the FlashPlate kit detection buffer. The assay is then incubated for an additional 3 h at room temperature, and bound radioactivity is measured using a liquid scintillation counter. cAMP levels are determined as per manufacturer’s instructions. For Schild Plot analysis, aliquots of cells are preincubated with 56, 100, 178, 300, 560, and 1000 nM 9m for 30 min at room temperature prior to the addition of 0.001-1000 nM glucagon to initiate the assay. Data are analyzed using the linear and nonlinear regression analysis software GraphPad Prism, v4. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

588.48

Formula

C₃₂H₂₇Cl₂N₃O₄

CAS No.

870823-12-4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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MK 0893
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HY-50663
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