Amfenac Sodium Monohydrate

製品コードS4149 バッチS414901

印刷

化学情報

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

C15H12NO3.H2O.Na
分子量 295.27 CAS No. 61618-27-7
Solubility (25°C)* 体外 DMSO 59 mg/mL (199.81 mM)
Water 59 mg/mL (199.81 mM)
Ethanol 4 mg/mL (13.54 mM)
* <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 Amfenac Sodium monohydrate is a non-steroidal analgesic anti-inflammatory drug with acetic acid moiety. The IC50 values for COX1 and COX2 is 250 nM and 150 nM, respectively.
in vitro Amfenac is a potent inhibitor of both COX-1 and COX-2 with IC50 of 0.25 and 0.15 μM. [1]
in vivo Amfenac possesses both antipyretic and analgesic properties in vivo. Amfenac (4 mg/kg) suppressed acute (Evans blue-carrageenan pleural effusion) and chronic (adjuvant-induced arthritis) inflammation by 33% and 28%, respectively, which is 16.4 and 22.8 times more potent than phenylbutazone. The analgesic activity of Amfenac is 43 times that of acetylsalicylic acid in the Randall-Selitto assay, and 156 and 56.3 times more potent than phenylbutazone in the acetylcholine-induced abdominal constriction in mice and in the bradykinin-induced nociceptive response in dogs, respectively. Amfenac produces less gastric irritation than acetylsalicylic acid when applied topically to the exposed gastric mucosa of cats or when administered orally to rats and dogs. Upon subchronic oral administration to rats, the therapeutic ratio of Amfenac is twice that of phenylbutazone. [2]

プロトコル(参考用のみ)

キナーゼアッセイ PGH synthase activity
Inhibition of PGH synthase activity from sheep vesicular glands (COX-1) is assayed polarographically with a YSI model 53 oxygen monitor. 10 μL of solubilized microsomal preparation ( 20 mg/mL) is added to the YSI incubation chamber containing 3.0 mL of 50 mM phosphate buffer (pH 7.4), 0.5 mM phenol, and 0.5 mM hematin. Aliquots (≤ 50 mL) of carrier or test compound dissolved in DMSO (carrier) are added to the chamber which is pre-equilibrated to 30 ℃. The mixture is stirred for two minutes before the reaction is initiated by addition of 30 mL of ammonium arachidonate (10 mM).

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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