1360550-05-5
1360550-05-5 structure
- Name: (S)-BI 665915
- Chemical Name: (S)-BI 665915
- CAS Number: 1360550-05-5
- Molecular Formula: C24H26N8O2
- Molecular Weight: 458.52
- Catalog: Signaling Pathways Immunology/Inflammation FLAP
- Create Date: 2020-01-23 19:11:51
- Modify Date: 2024-01-14 08:03:04
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(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 drug metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production[1].
| Name | (S)-BI 665915 |
|---|
| Description | (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 drug metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production[1]. |
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| Related Catalog | |
| Target |
IC50: 1.7 nM (FLAP) and 45 nM (FLAP functional in human whole blood)[1] |
| In Vitro | (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]. |
| In Vivo | (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 (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[1]. Animal Model: C57BL/6 mice[1] 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[1] 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. |
| References |
| Molecular Formula | C24H26N8O2 |
|---|---|
| Molecular Weight | 458.52 |