MK-5596

Cat. No.: HY-10575: Data Sheet Handling Instructions
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MK-5596 is an efficient, selective and orally active CB1R (IC₅₀ = 1.0 nM, EC₅₀ = 5.8 nM) inverse agonist. MK-5596 has weak hERG inhibitory activity. MK-5596 has strong weight loss and appetite suppression effects. MK-5596 has a certain inhibitory effect on CYP enzymes (CYP3A4: IC₅₀ = 3.3 μM, CYP2C8: IC₅₀ = 11 μM, CYP2C9: IC₅₀ = 18 μM, CYP2D6: IC₅₀ = 6 μM). MK-5596 can be used for research on conditions such as obesity.

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

MK-5596 Chemical Structure

CAS No. : 1044586-68-6

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•Related Small Molecules:

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View All Cannabinoid Receptor Isoform Specific Products:

View All Isoforms

CB1 CB2

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms

CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

CB1

1.0 nM (IC₅₀)

CYP3A4

3.3 μM (IC₅₀)

CB1

5.8 nM (EC₅₀)

CYP2C8

11 μM (IC₅₀)

CYP2C9

18 μM (IC₅₀)

CYP2D6

6 μM (IC₅₀)

Molecular Weight

541.86

Formula

C₂₇H₂₃Cl₃N₄O₂

CAS No.

1044586-68-6

SMILES

ClC1=CC=C(C2=CC3=C(OC(C)(C)C[C@H]3NC(C4=NNC(C)=C4)=O)N=C2C5=C(Cl)C=C(Cl)C=C5)C=C1

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]. Yan L, et al. Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity. J Med Chem. 2010 May 27;53(10):4028-37. [Content Brief]

MK-5596 Related Classifications

Metabolic Disease

Molarity Calculator
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The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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-55961044586-68-6MK5596MK 5596Cannabinoid ReceptorCytochrome P450CYPsCB1RhERGCYPobesityInhibitorinhibitorinhibit

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