MK 0893

Name: MK 0893
Brand: MedChemExpress
SKU: HY-50663
Rating: 5.0 (6 reviews)

Cat. No.: HY-50663 Purity: 99.83%: Data Sheet
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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.

CAS No. : 870823-12-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 6 publication(s) in Google Scholar

6 Publications Citing Use of MCE MK 0893

Bio/Physico-chemical Assay

Cell Imaging/Staining

Cell Proliferation/Viability Assay

: MK 0893 purchased from MedChemExpress. Usage Cited in: Preprints. 2024 Mar 25.; MK 0893 (5 nM; 2 h) significantly reversed the significant reduction in cell viability seen after GIPR overexpression in the retinoblastoma cell lines Weri.

: MK 0893 purchased from MedChemExpress. Usage Cited in: Endocrinology. 2021 Apr 1;162(4):bqab022. [Abstract]; MK 0893 (10 μM) significantly increased the uptake of the fluorescently labelled cholesterol in primary human ileal crypt cultures.

: MK 0893 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Mar 8;294(10):3514-3531. [Abstract]; MK 0893 (1-30 μM) reduced the dose-dependent actions of glucagon and GLP-1 to raise levels of cAMP in INS-1 832/13 cells.

: MK 0893 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Mar 8;294(10):3514-3531. [Abstract]; MK 0893 (3-30 µM) dose-dependently inhibited the action of glucagon (1 nM) in HEK293-GluR cells transduced with H188.

: MK 0893 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2019 Mar 8;294(10):3514-3531. [Abstract]; MK 0893 (1-30 μM) inhibited the actions of glucagon (1 nM) and GLP-1 (300 pM) in HEK293-GLP-1R cells transduced with H188.

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Biological Activity
Protocol
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References
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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)

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	1019 nM Compound: 9m, MK0893	Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at human GIPR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	104.5 nM Compound: 9m, MK0893	Antagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at dog GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	122 nM Compound: 9m, MK0893	Antagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at mouse GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	12800 nM Compound: 9m, MK0893	Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at human VPAC2 expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	15.7 nM Compound: 9m, MK0893	Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at human GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	55.5 nM Compound: 9m, MK0893	Antagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at rhesus monkey GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	6.6 nM Compound: 9m, MK0893	Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay Displacement of [125I]glucagon from human GCGR expressed in CHO cells after 3 hrs by scintillation proximity assay	[PMID: 22708876]
CHO	IC₅₀	727 nM Compound: 9m, MK0893	Antagonist activity at rat GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at rat GCGR expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
CHO	IC₅₀	> 10000 nM Compound: 9m, MK0893	Antagonist activity at human GLP1R expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at human GLP1R expressed in CHO cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
HT-29	IC₅₀	11580 nM Compound: 9m, MK0893	Antagonist activity at human VPAC1 expressed in HT-29 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at human VPAC1 expressed in HT-29 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]
NIH3T3	IC₅₀	9200 nM Compound: 9m, MK0893	Antagonist activity at human PAC1 expressed in mouse HIN 3T3 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter Antagonist activity at human PAC1 expressed in mouse HIN 3T3 cells assessed as inhibition of glucagon-induced cAMP accumulation preincubated for 30 mins prior to glucagon challenge measured after 30 mins post glucagon challenge by liquid scintillation counter	[PMID: 22708876]

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.

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.

870823-12-4

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
10 mM	0.1699 mL	0.8496 mL	1.6993 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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: 99.83%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (254 KB) HNMR (149 KB) RP-HPLC (162 KB) NP-HPLC (126 KB) LCMS (234 KB)

Handling Instructions (2659 KB)

References

[1]. Xiong Y, et al. Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.J Med Chem. 2012 Jul 12; [Content Brief]

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

[1]. Xiong Y, et al. Discovery of a novel glucagon receptor antagonist N-[(4-{(1S)-1-[3-(3, 5-dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)carbonyl]-β-alanine (MK-0893) for the treatment of type II diabetes.J Med Chem. 2012 Jul 12; [Content Brief]

Complete Stock Solution Preparation Table

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

MK 0893 Related Classifications

Metabolic Disease

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

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MK 0893

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MK 0893 Related Antibodies

6 Publications Citing Use of MCE MK 0893

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