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包装规格:5g 25g 100g in glass bottle
溶解性:溶于DMSO(14.29 mg/mL 超声)
产品描述:基本信息 产品编号:N10419 产品名称:Nevirapine CAS: 129618-40-2   储存条件 粉末 2-8℃ 四年     分子式: C15H14N4O 溶于液体 -80℃ 两年 分子量 266.30 -20℃ 一个月 化学名:  11-CYCLOPROPYL-5,11-DIHYDRO-4-METHYL-6H-DIPYRIDO[3,2-B:2',3'-E][1,4]DIAZEPIN-6-ONE   Solubility (25°C)   体外 DMSO 53mg/mL (199.02mM) Ethanol Insoluble Water Insoluble 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 3.7552mL 18.7758mL 37.5516mL 5mM 0.7510mL 3.7552mL 7.5103mL 10mM 0.3755mL 1.8776mL 3.7552mL 50mM 0.0751mL 0.3755mL 0.7510mL   生物活性 产品描述 一种用于研究 HIV/AIDS 的 HIV-1 逆转录酶非核苷抑制剂,Ki 值为 270μM。 靶点/IC50 Reverse transcriptase   体外研究 Nevirapine itself is an inhibitor of only CYP3A4 at concentrations that are well above those of therapeutic relevance (Ki=270μM). Nevirapine has been used as a re-differentiation agent to treat cancers in several human cancer models. At all doses(100, 200, 350, 500μM) tested, nevirapinesignificantly inhibits cell proliferation after 48 h treatment. At high dose (500μM),nevirapine significantly increases the percentage of apoptotic cells compared with control. Nevirapine is a potent andselective inhibitor (IC50=10-100nM) of the replication of a wide variety of HIV-1 strains in several cellular assays.   体内研究 Nevirapine is available for use in combination with nucleoside HIV-1 reverse transcriptase inhibitors (e.g., zidovudine,didanosine, etc.). Nevirapine has received FDA approval for use in combination with HIV-1 protease inhibitors (e.g.,saquinavir, ritonavir, indinavir, etc.). In humans, nevirapine is eliminated primarily in the urine as glucuronide conjugates of2-, 3-, 8-, and 12-hydroxynevirapine. Nevirapine is completely absorbed in both sexes of mouse, rat, rabbit, monkey, andchimpanzee. Nevirapine is extensively metabolized in both sexes of all animal species studied. Nevirapine (9mg/kg, 18mg/kg and 36mg/kg) shows significant reduction in ulcer severity score and ulcer index as compared to the control   推荐实验方法(仅供参考) 细胞实验:   Cell Assay FRO cells are seeded into 96-well culture plates at 10,000 cells/well. Cells are treated with different doses of nevirapine (0,100, 200, 350 and 500μM) for 48h. MTT dye (5mg/mL) is added to each well for additional 4h, and the reaction is thenstopped by the addition of DMSO. Optical density is measured at 490nm on a multi-well plate reader.     动物实验:   Animal Administration Rats: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1,v/v) with mildheating. The concentration of drug in suspension is 2mg/mL (20mg/kg, 26μCi) for oral dosing to rats and 6.7 mg/mL (20.3mg/kg, 10μCi males, 8.9μCi females) for intraduodenal administration to rats before bile collection. The i.v. dose isadministered to rats (1.1mg/kg, 20μCi) as a solution in 20% ethanol/80% saline.Mice: Nevirapine and [14C] Nevirapine are dissolved together in absolute ethanol and methylene chloride (1:1,v/v) with mildheating. The concentration of drug in suspension is 2mg/mL (20 mg/kg, 2.5μCi) with a specific activity of 5.55μCi/mg fororal dosing to mice
保存条件:2-8℃