T-226296

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T-226296 is an oral active and selective melanin-concentrating hormone receptor antagonist with the IC₅₀ values of 5.5 nM and 8.6 nM for human SLC-1 and rat SLC-1, respectively. T-226296 can be used for study of obesity and insulin resistance.

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

T-226296 Chemical Structure

CAS No. : 331758-35-1

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	14 nM Compound: 1h	Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting Displacement of [125I]-MCH from human MCHR1 expressed in CHO cells after 60 mins by scintillation counting	[PMID: 21856163]
CHO	IC₅₀	24 nM Compound: 1h	Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting Displacement of [125I]-MCH from rat MCHR1 expressed in CHO cells after 60 mins by scintillation counting	[PMID: 21856163]
CHO	IC₅₀	43 nM Compound: 1h	Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting Antagonist activity at human MCHR1 expressed in CHO cells assessed as inhibition of MCH-induced GTPgammaS binding after 60 mins by scintillation counting	[PMID: 21856163]
CHO	IC₅₀	5.5 nM Compound: 1, T-226296	Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay Displacement of [125I]MCH from human MCHR1 expressed in CHO cells by competition binding assay	[PMID: 21190859]
HEK293	IC₅₀	5.5 nM Compound: I, T-226296	Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay Antagonist activity at CART form of human MCH1 receptor expressed in HEK293 cells coexpressing Galphaq assessed as inhibition of MCH-induced intracellular calcium level by FLIPR assay	[PMID: 19773162]
IMR-32	IC₅₀	872 nM Compound: T-226296 (-)	Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader Concentration required to inhibit 50% of melanin-concentrating hormone induced [Ca2+] flux in IMR-32 cells measured by using a fluorometric imaging plate reader	[PMID: 15341943]

Molecular Weight

402.50

Formula

C₂₆H₂₇FN₂O

CAS No.

331758-35-1

SMILES

O=C(C1=CC=C(C2=CC=C(C=C2)F)C=C1)NC3=CC=C(CC(CC4)CN(C)C)C4=C3

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]. Takekawa S, et al. T-226296: a novel, orally active and selective melanin-concentrating hormone receptor antagonist. Eur J Pharmacol. 2002;438(3):129-135. [Content Brief]

T-226296 Related Classifications

Metabolic Disease

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

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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:

T-226296331758-35-1T226296T 226296MCHR1 (GPR24)Melanin concentrating hormone receptor 1CHO cells，obesityinsulin resistanceInhibitorinhibitorinhibit

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