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BMS-819881
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。
BMS-819881图片
CAS NO:1197420-05-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
BMS-819881 是一种黑色素浓缩激素受体1 (MCHR1) 拮抗剂,结合大鼠 MCHR1,Ki值为 7 nM。BMS-819881 还有效且选择性地作用于CYP3A4EC50为 13 μM。
生物活性

BMS-819881 is a melaninconcentrating hormone receptor 1 (MCHR1) antagonist, which binds ratMCHR1with aKiof 7 nM. BMS-819881 also is selective and potent forCYP3A4activity with anEC50of 13 μM.

IC50& Target[1]

CYP3A4

13 μM (EC50)

rat MCHR1

7 nM (Ki)

体外研究
(In Vitro)

BMS-819881 (Compound 27) is 99.8% binds to rat serum proteins and rat MCHR1 Kiis 7 nM. FLIPR-based assays establish that BMS-819881 is a potent and highly selective MCHR1 functional antagonist. BMS-819881 (Kb=32 nM) effectively blocks MCH stimulated Ca2+mobilization in heterologous cells overexpressing MCHR1 but fails to inhibit MCH mediated Ca2+mobilization of cells expressing MCHR2 at 10 μM. No activity is observed upon screening BMS-819881 at 10 μM versus a panel of 20 GPCRs associated with feeding homeostasis. The percent of BMS-819881 binds to serum proteins is species dependent ranging from 99.8%, 99.6%, and 99.3%, respectively, for rat, dog, and monkey. When BMS-819881 is screened for cytochrome P450 (CYP) activity, EC50values for CYP1A2, CYP2C9, CYP2C19, CYP2D6 are >40 μM; however, the CYP3A4 EC50is 13 μM[1].

体内研究
(In Vivo)

BMS-819881 has moderate terminal elimination half-life (t1/2=5.7 h, 32±8 h, and 14±3 h for rat (1 mg/kg, iv), dog (1 mg/kg, iv), and cynomologous monkey (1 mg/kg, iv))[1].

分子量

468.95

Formula

C24H21ClN2O4S

CAS 号

1197420-05-5

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.