(S)-BI 665915 is an orally active oxadiazole-containing5-lipoxygenase-activating protein (FLAP)inhibitor with anIC₅₀of 1.7 nM forFLAPbinding. (S)-BI 665915 inhibitsFLAPfunctional in human whole blood with anIC₅₀of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species drug metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition ofLTB₄production^[1].

IC50: 1.7 nM (FLAP) and 45 nM (FLAP functional in human whole blood)^[1]

(S)-BI 665915 shows significantly weaker activity in mouse whole blood (mWB) assay than in human whole blood (mWB IC₅₀=4800 nM; hWB IC₅₀=45 nM)^[1].
(S)-BI 665915 shows a modest human hepatocyte clearance (41% percent of hepatic blood flow) and relatively high plasma protein binding (unbound fraction of 4.7%)^[1].

(S)-BI 665915 (oral; 1-100 mg/kg) demonstrates dose-dependent LTB4 production inhibition in mouse whole blood, 2 h after single oral dose^[1].
(S)-BI 665915 (iv of 1 mg/kg or po of 10 mg/kg) shows low iv plasma clearance in all three species, with clearance values of 7 % Qh in rat, 2.8 % Qh in dog, and 3.6 % Qh in cynomolgus monkey, respectively. The volume of distribution (V_ss) across species tested is in a range of 0.5 to 1.2 L/kg, and the bioavailability was good (45 to 63 %) in all species tested^[1].

458.52

C₂₄H₂₆N₈O₂

1360550-05-5

Room temperature in continental US; may vary elsewhere.

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