SB-649868 是一种有效的选择性口服活性食欲素拮抗剂，对 OX1 和 OX2 受体的 pKi 分别为 9.4 和 9.5。

SB-649868 is a potent and selective orally active antagonist of orexin(pKi =9.4 and 9.5 at the OX1 and OX2 receptor, respectively).

SB-649868 antagonizes orexin-A-induced inositol 1 phosphate (IP1) accumulation with the following pKB value (OX1=9.67;?OX2=9.64).?SB-649868 displaces the [3H]ACT-078573 receptor binding with the following pKi values: OX1=9.27;?OX2=8.91.?Increasing concentrations of SB-649868 (0.3 nM-30 nM) induces a rightward shift of the orexin-A CRCs with a depression of the agonist efficacy suggesting a clear non-surmountable behavior.?The calculated apparent pKb values are 9.67 0.03 and 9.64 0.07 for OX1 and OX2

380899-24-1

C26H24FN3O3S

477.55

GSK649868

DMSO:100 mg/mL (209.40 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years