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Cat. No.: HY-11073

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MK-0489

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.

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CAS No.: 778625-65-3
Formule: C₃₄H₄₄ClF₂N₃O₂
Masse moléculaire:600.18

Stockage:

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

Data Sheet (276 KB)

MK-0489 Chemical Structure

CAS No.: 778625-65-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]

MC4R

Voir tous les produits spécifiques à Isoform Melanocortin Receptor :

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.

Chemical Information

CAS No. 778625-65-3
Masse moléculaire 600.18
Formule C₃₄H₄₄ClF₂N₃O₂
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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (276 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[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]

Calculators

Calculateur de molarité

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Calculateur de dilution

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vivo
Chemical Information
Pureté et documentation
Références

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MK-0489

Voir tous les produits spécifiques à Isoform Melanocortin Receptor

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

MK-0489 Related Classifications

HY-11073 Related Classifications