MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Fiboflapon

CAS No. : 936350-00-4

MCE 站：Fiboflapon

产品活性：Fiboflapon (GSK2190915; AM-803) 是一种口服有效的 5-脂氧合酶激活蛋白 (FLAP) 抑制剂，结合 FLAP 的效价为 2.9 nM，在人血中抑制 LTB4 的 IC₅₀ 为 76 nM。

研究领域：Immunology/Inflammation  |  GPCR/G Protein

作用靶点：FLAP  |  Leukotriene Receptor

In Vitro: Fiboflapon (AM-803) exhibits excellent preclinical toxicology and pharmacokinetics in rat and dog. Fiboflapon (AM-803) also demonstrated an extended pharmacodynamic effect in a rodent bronchoalveolar lavage (BAL) model [1].

In Vivo: Oral administration of Fiboflapon (AM-803: 1 mg/kg) results in sustained inhibition of ex vivo ionophore-challenged whole blood LTB4 biosynthesis with >90% inhibition for up to 12 h and an EC₅₀ of approximately 7 nM. When rat lungs are challenged in vivo with calcium-ionophore, Fiboflapon (AM-803) inhibits LTB4 and cysteinyl leukotriene (CysLT) production with ED₅₀s of 0.12 mg/kg and 0.37 mg/kg, respectively. The inhibition measured 16 h following a single oral dose of 3 mg/kg was 86% and 41% for LTB4 and CysLTs, respectively. In an acute inflammation setting, Fiboflapon dose-dependently reduced LTB4, CysLTs, plasma protein extravasation and neutrophil influx induced by peritoneal zymosan injection. Finally, Fiboflapon increases survival time in mice exposed to a lethal intravenous injection of platelet activating factor (PAF).

相关产品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  GPCR/G Protein Compound Library  |  Immunology/Inflammation Compound Library  |  Clinical Compound Library  |  Drug Repurposing Compound Library  |  Anti-COVID-19 Compound Library  |  Orally Active Compound Library  |  MK-571 sodium salt  |  Montelukast sodium  |  MK-886  |  Zafirlukast  |  Quiflapon  |  Pranlukast  |  Nedocromil  |  AM679  |  LY223982  |  CP-105696  |  HAMI 3379  |  Leukotriene B4  |  LY255283  |  (S)-Verapamil hydrochloride  |  5-O-Demethylnobiletin  |  BIIL-260 hydrochloride  |  Etalocib  |  11-?Keto-?beta-?boswellic acid  |  12S-HHT  |  AS-35  |  Darbufelone  |  KP496  |  RG-12525  |  Veliflapon  |  CP-96021 hydrochloride

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。