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

BMS-819881 (Compound 27) is 99.8% binds to rat serum proteins and rat MCHR1 K_iis 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, EC₅₀values for CYP1A2, CYP2C9, CYP2C19, CYP2D6 are >40 μM; however, the CYP3A4 EC₅₀is 13 μM^[1].

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))^[1].

468.95

C₂₄H₂₁ClN₂O₄S

1197420-05-5

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.