(S)-BI 665915
(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.
For research use only. We do not sell to patients.
The (S)-BI 665915 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- CAS No.: 1360550-05-5
- Formula: C24H26N8O2
- Molecular Weight:458.52
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
(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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
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.
Chemical Information
-
CAS No. 1360550-05-5
-
Molecular Weight 458.52
-
Formula C24H26N8O2
-
SMILES
O=C(N(C)C)CN1N=CC(C2=NC([C@@](C3CC3)(C4=CC=C(C5=CN=C(N)N=C5)C=C4)C)=NO2)=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Takahashi H, et al. Synthesis, SAR, and series evolution of novel oxadiazole-containing 5-lipoxygenase activating protein inhibitors: discovery of 2-[4-(3-{(r)-1-[4-(2-amino-pyrimidin-5-yl)-phenyl]-1-cyclopropyl-ethyl}-[1,2,4]oxadiazol-5-yl)-pyrazol-1-yl]-N,N-dimethyl-acetamide (BI 665915). J Med Chem. 2015 Feb 26;58(4):1669-90. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(S)-BI 665915 Related Classifications
HY-12995A Related Classifications
Powered by Bioz