Ossirene (AS101)

製品コードS8301 バッチS830102

印刷

化学情報

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

C2H4Cl3O2Te.H4N
分子量 312.05 CAS No. 106566-58-9
Solubility (25°C)* 体外 DMSO 62 mg/mL (198.68 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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 強力なin vitroおよびin vivoの免疫調節剤であるOssirene（AS101）は、IL-1beta converting enzymeの新規阻害剤です。
in vitro Treatment of caspase-1 (interleukin-1 [IL-1] converting enzyme [ICE]) with Ossirene (AS101) inhibits its enzymatic activity in a dose-dependent manner. Moreover, it causes a significant reduction in the active form of IL-18 and IL-1 in peripheral blood mononuclear cells (PBMC) and in human HaCat keratinocytes. The inhibitory effect of this compound does not involve nitric oxide (NO) or interferon- (IFN- ), two possible regulators of IL-18 production, and does not occur at the mRNA level. It may exert effects through a posttranscriptional mechanism. AS101 induced SIRT1 expression in a dose dependent manner in three different cell lines, HEK293, HL-60 and Rin-5f. Incubation of HEK293 and HL-60 cell lines with it (0.1-2.5μg/ml) resulted in a dose dependent reduction in PPARγ protein expression relative to the control cells, and the reduction of PPARγ expression is in parallel to increased SIRT1 expression.
in vivo Ossirene (AS101) downregulates IL-18 and IL-1 serum levels in a mouse model of lipopolysaccharide (LPS)-induced sepsis, resulting in increased survival. It has also been shown to be protective against lethal and sublethal effects of irradiation and chemotherapy. In a model of cecal ligation and puncture (CLP)-induced sepsis in mice, this compound also exerted beneficial effects. Treated rats showed a large increase in SIRT1 protein levels in the liver and kidney extracts. It prevents development of insulin resistance in vivo and affects SIRT1 related metabolic pathways by changing the insulin levels. AS101 treatment prevents hyperglycemia associated with T2D(type 2 diabetes) and some of the symptoms of the disease in the HFD(high fat diet)+STZ(Streptozotocin) rat model.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Human peripheral blood mononuclear cells (PBMC)
濃度 0.01, 0.05, 0.5, 1, 1.5, 2 μg/mL
反応時間 24 h
実験の流れ

PBMCs were first treated with various concentrations of Ossirene (AS101). After 1 h, SAC (10-3 v/v) was added to this compound. After 24 h, supernatants were collected and evaluated for cytokine content.
動物実験 動物モデル c57BL/6J and BALB/c mice
投薬量 10 μg/mouse
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/17572009/
  • https://pubmed.ncbi.nlm.nih.gov/22761194/

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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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