Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fiboflapon sodium (GSK2190915) is an orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
2 mg | 約 5 days | ¥ 20,500 |
25 mg | 約8-10 週間 | ¥ 146,000 |
50 mg | 約8-10 週間 | ¥ 189,500 |
100 mg | 約8-10 週間 | ¥ 284,500 |
ターゲット&IC50 | LTB4:76 nM |
In vitro | In vivo studies revealed that Fiboflapon (AM803) effectively inhibits the production of LTB4 and cysteinyl leukotriene (CysLT) in rat lungs challenged with calcium-ionophore, showing ED50 values of 0.12 mg/kg and 0.37 mg/kg, respectively. Following a single oral dose of 3 mg/kg, inhibition levels 16 hours post-administration were 86% for LTB4 and 41% for CysLTs. In scenarios of acute inflammation, Fiboflapon (AM803) demonstrated a dose-dependent reduction in LTB4, CysLTs, plasma protein extravasation, and neutrophil influx following peritoneal zymosan injection. Furthermore, AM803 significantly prolonged survival in mice after a lethal dose of platelet-activating factor (PAF) intravenously. Fiboflapon (AM803) has shown excellent preclinical toxicology and pharmacokinetics in rats and dogs, alongside a remarkable pharmacodynamic extension in a rodent bronchoalveolar lavage (BAL) model. Oral administration at 1 mg/kg led to a sustained inhibition of LTB4 biosynthesis in ex vivo ionophore-challenged whole blood, with over 90% inhibition lasting up to 12 hours and an EC50 of approximately 7 nM. |
別名 | GSK2190915 sodium salt, AM-803 sodium |
分子量 | 660.83 |
分子式 | C38H43N3NaO4S |
CAS No. | 1196070-26-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 32 mg/mL (48.50 mM)
You can also refer to dose conversion for different animals. 詳細
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Fiboflapon sodium 1196070-26-4 Immunology/Inflammation LTR GSK2190915 sodium salt GSK2190915 sodium AM-803 sodium Inhibitor inhibitor inhibit