BMS-819881,1197420-05-5

价格￥3960

品牌MedChemExpress(MCE)
产地美国
货号HY-12433
更新日期2025年12月05日

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BMS-819881

CAS No. : 1197420-05-5

MCE 国际站：BMS-819881

产品活性：BMS-819881 是一种黑色素浓缩激素受体1 (MCHR1) 拮抗剂，结合大鼠 MCHR1，K_i 值为 7 nM。BMS-819881 还有效且选择性地作用于 CYP3A4，EC₅₀ 为 13 μM。

研究领域：GPCR/G Protein | Neuronal Signaling | Metabolic Enzyme/Protease

作用靶点：MCHR1 (GPR24) | Cytochrome P450

In Vitro: BMS-819881 (Compound 27) is 99.8% binds to rat serum proteins and rat MCHR1 K_i is 7 nM. FLIPR-based assays establish that BMS-819881 is a potent and highly selective MCHR1 functional antagonist. BMS-819881 (K_b=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, EC₅₀ values for CYP1A2, CYP2C9, CYP2C19, CYP2D6 are >40 μM; however, the CYP3A4 EC₅₀ is 13 μM.

In Vivo: BMS-819881 has moderate terminal elimination half-life (t_1/2=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)).