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

(S)-BI 665915 是一种口服有效的,含恶二唑的 5-脂氧合酶激活蛋白 (FLAP) 抑制剂,与 FLAP 结合的 IC50 为 1.7 nM。(S)-BI 665915 抑制人全血中 FLAP 功能,IC50 为 45 nM。(S)-BI 665915 展示了极好的跨物种活性分子代谢和药代动力学 (DMPK) 谱以及对 LTB4 产生的剂量依赖性抑制。

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(S)-BI 665915 Chemical Structure

(S)-BI 665915 Chemical Structure

CAS No. : 1360550-05-5

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

IC50: 1.7 nM (FLAP) and 45 nM (FLAP functional in human whole blood)[1]

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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].

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.
分子量

458.52

Formula

C24H26N8O2

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献

(S)-BI 665915 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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