Fenspiride HCl

製品コードS4090 バッチS409001

印刷

化学情報

 Chemical Structure Synonyms Decaspiride Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C15H20N2O2.HCl

分子量 296.79 CAS No. 5053-08-7
Solubility (25°C)* 体外 Water 59 mg/mL (198.79 mM)
DMSO 9 mg/mL (30.32 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Fenspiride(Decaspiride) is a bronchodilator with anti-inflammatory properties, inhibiting phosphodiesterase 4 and phosphodiesterase 3 activities with logIC50 values of 4.16 and 3.44, respectively, in human isolated bronchi.
in vitro

Fenspiride induces potentiation of the effects of isoprenaline and sodium nitroprusside with logEC50 of 4.1 and 3.5, respectively, in human isolated bronchi. [1]

in vivo

Fenspiride, an antiinflammatory drug with low anti-cyclooxygenase activity, administered orally at 60-200 mg/kg inhibits neutrophil migration into peritoneal and air pouches cavities as well as exudation into peritoneal cavities induced by endotoxin but not induced by carrageenin in the rat. Fenspiride (200 mg/kg) inhibits the release of tumour necrosis factor by stimulated macrophages in a dose-dependent manner in the rat. [2] Fenspiride (Topically applied) is found to inhibit the development of sclerotic lesions in myringotomized rats, whereas intraperitoneal injections are ineffective. [3] Fenspiride (60 mg/kg) significantly reduces the lipopolysaccharide-induced early rise of tumor necrosis factor concentrations in serum (4.2 ng/mL vs. 2.3 ng/mL) and in the bronchoalveolar lavage fluid (55.7 ng/mL vs. 19.7 ng/mL) of guinea-pigs with endotoxemia. Fenspiride (60 mg/kg) also significantly reduces the lipopolysaccharide-induced primed stimulation of alveolar macrophages, defined as their enhanced release of arachidonic acid metabolites as compared to cells from untreated controls upon stimulation with N-formyl-methionyl-phenylalanine. Fenspiride (60 mg/kg) reduces the increased serum concentrations of extracellular type II phospholipase A2, the intensity of the neutrophilic alveolar invasion and the lethality due to the lipopolysaccharide in guinea-pigs with endotoxemia. [4]

特徴 Produces less than 25% inhibition of phosphodiesterase 1 and phosphodiesterase 2 activities.

プロトコル(参考用のみ)

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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