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编 号：F683723
分子式：C24H26N8O2
分子量：458.52
分子式：C24H26N8O2
分子量：458.52
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CAS No: 1360550-05-5
产品详情
生物活性：
(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production.
体内研究：
(S)-BI 665915 (oral; 1-100 mg/kg) demonstrates dose-dependent LTB4 production inhibition in mouse whole blood, 2 h after single oral dose. (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. Animal Model:C57BL/6 mice
Dosage:1, 3, 10, 30, 100 mg/kg (Pharmacokinetic Analysis)
Administration:Oral
Result:Demonstrated dose-dependent LTB4 production inhibition in mouse whole blood, 2 h after single oral dose.
Animal Model:Rat; dog; cynomolgus monkey
Dosage:1 mg/kg (iv) or 10 mg/kg (po)
Administration:Iv or po
Result:Showed 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.
体外研究：
(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). (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%).
(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species agent metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production.
体内研究：
(S)-BI 665915 (oral; 1-100 mg/kg) demonstrates dose-dependent LTB4 production inhibition in mouse whole blood, 2 h after single oral dose. (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. Animal Model:C57BL/6 mice
Dosage:1, 3, 10, 30, 100 mg/kg (Pharmacokinetic Analysis)
Administration:Oral
Result:Demonstrated dose-dependent LTB4 production inhibition in mouse whole blood, 2 h after single oral dose.
Animal Model:Rat; dog; cynomolgus monkey
Dosage:1 mg/kg (iv) or 10 mg/kg (po)
Administration:Iv or po
Result:Showed 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.
体外研究：
(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). (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%).
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