NIM811  ≥98%

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包装规格:1mg in glass bottle
溶解性:溶于DMSO(≥ 100 mg/mL)
产品描述:基本信息 产品编号:N10413 产品名称:NIM811 CAS: 143205-42-9   储存条件 粉末 -20℃ 四年     分子式: C62H111N11O12 溶于液体 -80℃ 六个月 分子量 1202.61 -20℃ 一个月 化学名:  9-(N-Methyl-L-isoleucine)cyclosporin A   Solubility (25°C)   体外 DMSO 200mg/mL (166.30mM;Need ultrasonic) Ethanol   Water   体内 现配现用   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 0.8315mL 4.1576mL 8.3152mL 5mM 0.1663mL 0.8315mL 1.6630mL 10mM 0.0832mL 0.4158mL 0.8315mL   生物活性 产品描述 一种具有口服活性的线粒体渗透转换和亲环蛋白双抑制剂,对丙型肝炎病毒具有很强的体外活性。 靶点/IC50 Cyclophilin Mitochondrial Permeability Transition Inhibitor 体外研究 NIM811 induces a concentration-dependent reduction of HCV RNA in the replicon cells with an IC50 of 0.66μM at 48 h. In addition, the combination of NIM811 with alpha IFN significantly enhances anti-HCV activities without causing any increase of cytotoxicity. NIM811 blocks the mitochondrial permeability transition induced by calcium and inorganic phosphate. 体内研究 NIM811 prevents mitochondrial depolarization thereby attenuates liver injury, stimulates regeneration and improves liver function and survival.   推荐实验方法(仅供参考) 细胞实验:   Cell Assay The antiviral activity and cytotoxicity of compounds are determined using an HCV replicon cell line (Huh-Luc/neo-ET) containing a luciferase reporter gene. Briefly, 5,000 replicon cells are seeded in each well of 96-well tissue culture plates and are allowed to attach in complete culture medium without G418 overnight. On the next day, the culture medium is replaced with medium containing serially diluted NIM811 in the presence of 10% FBS and 0.5% DMSO. After a 48-h NIM811 treatment,the remaining luciferase activities in the cells are determined.   动物实验:   Animal Administration Mice: Male C57BL/6 mice (8-12 weeks) are gavaged with NIM811, 10 mg/kg or an equal volume of vehicle containing 8.3% polyethoxylated castor oil and 8.3% ethanol at 2 h before surgery. Mice undergo massive hepatectomy or sham-operation under ether anesthesia. NIM811 (5 mg/kg) or vehicle is gavaged daily post-operatively for 2 days. Mice are observed for 21 days for survival.
保存条件:-20℃