1. Immunology/Inflammation
  2. FLAP
  3. (S)-BI 665915

(S)-BI 665915 

Cat. No.: HY-12995A
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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.

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(S)-BI 665915 Chemical Structure

(S)-BI 665915 Chemical Structure

CAS No. : 1360550-05-5

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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].

IC50 & 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.
Molecular Weight

458.52

Formula

C₂₄H₂₆N₈O₂

CAS No.

1360550-05-5

SMILES

O=C(N(C)C)CN1N=CC(C2=NC([[email protected]@](C3CC3)(C4=CC=C(C5=CN=C(N)N=C5)C=C4)C)=NO2)=C1

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Storage

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

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Keywords:

(S)-BI 665915FLAP5-lipoxygenase-activating protein5-LO activating proteinorallyoxadiazole-containing5-lipoxygenase-activatingproteincross-speciesmetabolismpharmacokineticsDMPKLTB4Inhibitorinhibitorinhibit

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