2. GPCR/G Protein
  3. GCGR
  4. MK 0893

MK 0893 

Cat. No.: HY-50663 Purity: 99.86%
COA Handling Instructions

MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM.

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
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 489 In-stock
Solution
10 mM * 1 mL in DMSO USD 489 In-stock
Solid
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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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

MK 0893 Related Antibodies

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Description

MK 0893 is a potent and selective glucagon receptor antagonist with an IC50 of 6.6 nM.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MK 0893 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

588.48

Appearance

Solid

Formula

C32H27Cl2N3O4
CAS No.
SMILES

ClC1=CC(C2=NN(C(C3=CC4=C(C=C3)C=C(OC)C=C4)=C2)[C@H](C5=CC=C(C=C5)C(NCCC(O)=O)=O)C)=CC(Cl)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (56.64 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.25 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.86%

COA (254 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[1]

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
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MK 0893 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

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The dilution calculator equation

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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

MK 0893870823-12-4MK0893MK-0893GCGRGlucagon ReceptorInhibitorinhibitorinhibit

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