(S)-BI 665915

Name: (S)-BI 665915
Brand: TargetMol
SKU: T12793
Rating: 4.5 (1 reviews)

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产品编号 T12793Cas号 1360550-05-5

(S)-BI 665915 is an orally active inhibitor of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP)(IC50 of 1.7 nM for FLAP binding)..

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产品编号 T12793Cas号 1360550-05-5

(S)-BI 665915 is an orally active inhibitor of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP)(IC50 of 1.7 nM for FLAP binding)..

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生物活性

产品描述	(S)-BI 665915 is an orally active inhibitor of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP)(IC50 of 1.7 nM for FLAP binding)..
靶点活性	FLAP:1.7 nM , FLAP functional (human whole blood):45 nM
体外活性	(S)-BI 665915 shows significantly weaker activity in mouse whole blood (mWB) assay than in human whole blood (mWB with IC50 of 4800 nM; hWB with IC50 of 45 nM). (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%).
体内活性	(S)-BI 665915 (single oral dose; 1-100 mg/kg;2 h) demonstrates dose-dependent LTB4 production inhibition in mouse whole blood . (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 (Vss) 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.