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SB-568849
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SB-568849图片
CAS NO:395679-53-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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。
生物活性

SB-568849 is amelanin-concentrating hormone receptor 1(MCH R1) antagonist with apKiof 7.7.

IC50& Target

MCH R1 receptor[1]

体外研究
(In Vitro)

SB-568849 is a selective SLC-1 antagonist with a pKiof 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].

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 pKbof 7.7[3].

分子量

500.55

Formula

C28H31F3N2O3

CAS 号

395679-53-5

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.