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(S)-BI 665915

Catalog No. T12793 CAS 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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(S)-BI 665915, CAS 1360550-05-5

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,970.00
50 mg	8-10 weeks	$ 2,580.00
100 mg	8-10 weeks	$ 3,400.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	(S)-BI 665915 is an orally active inhibitor of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP)(IC50 of 1.7 nM for FLAP binding)..
Targets&IC50	FLAP:1.7 nM , FLAP functional (human whole blood):45 nM
In vitro	(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%).
In vivo	(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.

Molecular Weight	458.52
Formula	C24H26N8O2
CAS No.	1360550-05-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

(S)-BI 665915 1360550-05-5 Others BI 665915 (S) BI 665915 (S)BI 665915 BI-665915 BI665915 inhibitor inhibit

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