CAS NO: | 1197420-05-5 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
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] |
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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. |