2. GPCR/G Protein Neuronal Signaling
  3. MCHR1 (GPR24)
  4. T-226296

T-226296 是一种具有口服活性、选择性的黑色素浓缩激素受体 (melanin-concentrating hormone receptor) 拮抗剂，对人 SLC-1 和大鼠 SLC-1 的 IC50 值分别为 5.5 nM 和 8.6 nM。T-226296 可用于肥胖症和胰岛素抵抗的研究。

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T-226296 Chemical Structure

T-226296 Chemical Structure

CAS No. : 331758-35-1

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T-226296 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

细胞效力
(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]
分子量

402.50

Formula

C26H27FN2O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

T-226296 相关分类

  • 摩尔计算器

  • 稀释计算器

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

质量   浓度   体积   分子量 *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (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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产品名称：
T-226296
目录号：
HY-11085
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