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

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 (Highly Recommended)
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
1 mg USD 151 In-stock
5 mg USD 378 In-stock
10 mg USD 570 In-stock
50 mg USD 1400 In-stock
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

MK 0893 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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

Formula

C32H27Cl2N3O4
CAS No.
Appearance

Solid

Color

White to off-white

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6993 mL 8.4965 mL 16.9929 mL 42.4823 mL
5 mM 0.3399 mL 1.6993 mL 3.3986 mL 8.4965 mL
10 mM 0.1699 mL 0.8496 mL 1.6993 mL 4.2482 mL
15 mM 0.1133 mL 0.5664 mL 1.1329 mL 2.8322 mL
20 mM 0.0850 mL 0.4248 mL 0.8496 mL 2.1241 mL
25 mM 0.0680 mL 0.3399 mL 0.6797 mL 1.6993 mL
30 mM 0.0566 mL 0.2832 mL 0.5664 mL 1.4161 mL
40 mM 0.0425 mL 0.2124 mL 0.4248 mL 1.0621 mL
50 mM 0.0340 mL 0.1699 mL 0.3399 mL 0.8496 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

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.

Keywords:

MK 0893870823-12-4MK0893MK-0893GCGRGlucagon ReceptorInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
MK 0893
Cat. No.:
HY-50663
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.