1. GPCR/G Protein Neuronal Signaling
  2. MCHR1 (GPR24)
  3. SB-568849

SB-568849 是一种黑色素浓缩激素受体 1 (MCH R1) 拮抗剂,pKi 值为 7.7。

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SB-568849 Chemical Structure

SB-568849 Chemical Structure

CAS No. : 395679-53-5

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SB-568849 is a melanin-concentrating hormone receptor 1 (MCH R1) antagonist with a pKi of 7.7.

IC50 & Target

MCH R1 receptor[1]

体外研究
(In Vitro)

SB-568849 is a selective SLC-1 antagonist with a pKi of 7.7 as determined in radioligand binding displacement assays; coincubation of tissue with 1 μM SB-568849 for 45 min completely inhibits the MCH induced increase in corticotropin-releasing factor (CRF) release to basal levels without causing any effect on its own. The only reported MCH receptor in the rat is SLC-1, a G protein coupled receptor found throughout the brain and periphery[2].

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

体内研究
(In Vivo)

SB-568849 (Compound 15h) possesses good receptor affinity and selectivity. SB-568849 proves to be an antagonist with stability in vivo, an acceptable brain–blood ratio and oral bioavailability. SB-568849 retains affinity, demonstrates greater in vivo stability (CLb=16 mL/min/kg) and shows an acceptable brain-blood ratio of 1. SB-568849 also shows >30-fold selectivity over a wide range of monoamine receptors and is an antagonist in the FLIPR assay with a pKb of 7.7[3].

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

分子量

500.55

Formula

C28H31F3N2O3

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

This equation is commonly abbreviated as: C1V1 = C2V2

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  • 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.

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产品名称:
SB-568849
目录号:
HY-100308
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