Acemetacin

製品コードS2602 バッチS260202

印刷

化学情報

 Chemical Structure Synonyms K-708,TVX 1322 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C21H18ClNO6

分子量 415.82 CAS No. 53164-05-9
Solubility (25°C)* 体外 DMSO 83 mg/mL (199.6 mM)
Ethanol 83 mg/mL warmed with 50ºC water bath (199.6 mM)
Water 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 Acemetacin (K-708,TVX 1322) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
in vitro

Acemetacin is less potent than indomethacin in causing a concentration-related inhibition of PGE accumulation in gastric mucosal incubates. Acemetacin is also less potent than indomethacin in reducing gastric 6-keto-PGF1 alpha and TXB2. [1] Acemetacin probably exerts actions independent of conversion to Indomethacin, given the different effects of these two drugs on LTB(4) production. [2] Acemetacin is a prodrug of indomethacin that exhibits better gastric tolerability in preclinical and clinical trials. Acemetacin involves the sequential participation of nitric oxide (NO) or K+ channel pathways to confer its antinociceptive effect. [3] Acemetacin exhibits the anti-inflammatory effect through PG synthesis inhibition. Acemetacin prevents the PGE2 release only at the high concentration of 10 μM in inflamed synovial tissue. Acemetacin exhibits less potent inhibitory effect on PGE2 release from the synovial membrane in the in vitro study. [4]

in vivo

Acemetacin induces significantly less gastric and intestinal damage than indomethacin in rats pretreated with inhibitors of COX-2 and NOS, despite markedly suppressing COX activity. [5]

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。