MK-0489

Cat. No.: HY-11073: Data Sheet Handling Instructions
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MK-0489 is an orally active, highly effective, and selective MC4R agonist. MK-0489 exhibits a strong binding affinity (IC₅₀ = 13 nM) and functional agonist activity (EC₅₀ = 4.6 nM) at human MC4R. MK-0489 shows functional activity of 22 nM (EC₅₀) on mouse MC4R and 1.7 μM (EC₅₀) on mouse MC3R. MK-0489 can be used for the study of obesity.

For research use only. We do not sell to patients.

MK-0489 Chemical Structure

CAS No. : 778625-65-3

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MC1R MC3R MC2R MC4R MC5R

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References
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Description

IC₅₀ & Target^[1]

MC4R

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	1020 nM Compound: 1	Agonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at human MC1R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	EC₅₀	1020 nM Compound: 1r, MK-0489	Agonist activity at human MC1bR expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins Agonist activity at human MC1bR expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	[PMID: 20598882]
CHO	EC₅₀	2 nM Compound: 1	Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at rat MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	EC₅₀	22 nM Compound: 1	Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at mouse MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	EC₅₀	351 nM Compound: 1	Agonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at human MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	EC₅₀	4.6 nM Compound: 1r, MK-0489	Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins Agonist activity at human MC4R expressed in CHO cells assessed as increase of alpha-MSH-stimulated cAMP release pretreated for 10 mins before alpha-MSH challenge measured after 40 mins	[PMID: 20598882]
CHO	EC₅₀	4.9 nM Compound: 1	Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at human MC4R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	EC₅₀	997 nM Compound: 1	Agonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation Agonist activity at rat MC3R expressed in CHO cells assessed as stimulation of intracellular cAMP accumulation	[PMID: 20207541]
CHO	IC₅₀	13 nM Compound: 1	Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells Displacement of [125I]NDP-alpha-MSH from human MC4R expressed in CHO cells	[PMID: 20207541]
CHO	IC₅₀	13 nM Compound: 1r, MK-0489	Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting Displacement of [125I]-NDP-R-MSH from human MC4R expressed in CHO cells after 1.5 hrs by scintillation counting	[PMID: 20598882]
CHO	IC₅₀	1938 nM Compound: 1	Displacement of [125I]NDP-alpha-MSH from human MC1R expressed in CHO cells Displacement of [125I]NDP-alpha-MSH from human MC1R expressed in CHO cells	[PMID: 20207541]
CHO	IC₅₀	83.9 nM Compound: 1	Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells Displacement of [125I]NDP-alpha-MSH from human MC5R expressed in CHO cells	[PMID: 20207541]
CHO	IC₅₀	890 nM Compound: 1	Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells Displacement of [125I]NDP-alpha-MSH from human MC3R expressed in CHO cells	[PMID: 20207541]

In Vivo

MK-0489 (Compound 1r) (2-20 mg/kg, p.o., once or twice daily for 14 days) specifically reduces food intake and body weight in mice via MC4R-mediated reduction, and in a dose-dependent manner, it reduces body weight in a diet-induced obese rat model^[1].

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

Animal Model:	Wild type (WT) and MC4R/3R knockout (KO) mouse^[1].
Dosage:	10 mg/kg
Administration:	P.o., once
Result:	Significant reducted in food intake and body weight was observed in wild-type mice; however, no significant effect was observed in MC4R/3R knockout mice.

Animal Model:	Diet-induced obese rat model^[1].
Dosage:	2 mg/kg, 6 mg/kg, 20 mg/kg
Administration:	P.o., twice a day for 14 days
Result:	Exhibited dose-dependent weight loss effect.

Molecular Weight

600.18

Formula

C₃₄H₄₄ClF₂N₃O₂

CAS No.

778625-65-3

SMILES

CC(NC(C)([C@@H]1CC2(CCN(C([C@@H]3CN(C(C)(C)C)C[C@H]3C4=CC=C(F)C=C4F)=O)CC2)C5=C1C=C(C)C(Cl)=C5)C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. He S, et al. Spiroindane based amides as potent and selective MC4R agonists for the treatment of obesity. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4399-405. [Content Brief]

MK-0489 Related Classifications

Metabolic Disease

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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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-0489778625-65-3MK0489MK 0489Melanocortin ReceptorMC ReceptorMC4RAgonistObesityInhibitorinhibitorinhibit

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MK-0489

MK-0489 Related Antibodies

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Biological Activity

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MK-0489 Related Classifications

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