Thiocolchicoside

製品コードS5049 バッチS504902

印刷

化学情報

Chemical Structure Synonyms Thiocolchicine 2-glucoside analog, Coltramyl Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C27H33NO10S
分子量 563.62 CAS No. 602-41-5
Solubility (25°C)* 体外 DMSO 100 mg/mL (177.42 mM)
Water 33 mg/mL (58.55 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.

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生物活性

製品説明 Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) is a natural occuring glycoside originated from the flower seeds of superba gloriosa with anti-inflammatory and analgesic properties as well as pronounced convulsant activity. It is also an antagonist of GABAA receptor.
in vitro Thiocolchicoside exhibits a selective affinity for the inhibitory gamma-aminobutyric acid and glycinergic receptors. It has an agonistic action at the spinal-strychnine-sensitive receptors that could mediate its myorelaxant effect. It might preferentially interact with a cortical subtype of the gamma-aminobutyric acid type A (GABAA) receptor that expresses low-affinity binding sites for GABA. GABAB receptors are largely unaffected by thiocolchicoside and hence do not contribute to its muscle relaxation action. Thiocolchicoside suppresses osteoclastogenesis induced by receptor activator of nuclear factor kappa-B ligand, breast cancer and multiple myeloma cells through inhibition of inflammatory pathways[3].
in vivo Thiocolchicoside is used as muscle relaxant agent without any side effects. It is rapidly absorbed from the gastrointestinal tract, undergoes first pass metabolism with an oral bioavailability of about 25 % and a biological half-life of 5-6 h. Thiocolchicoside is broken down in the body to a metabolite called 3-demethylthiocolchicine that could damage cells therefore inducing toxicity in the embryo, neoplastic changes and fertility reduction in male. Local skin preparations are less toxic[1].

プロトコル(参考用のみ)

動物実験 動物モデル Male Sprague-Dawley CD rats
投薬量 10-30 mg/kg
投与方法 i.p.

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。