Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Efavirenz (DMP 266) 是一种人类免疫缺陷病毒 1 非核苷类似物逆转录酶抑制剂。它也是一种野生型HIV-1 RT 抑制剂,Ki 为 2.93 nM,有效抑制 HIV-1 复制,IC95为 1.5 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 313 | 现货 | ||
10 mg | ¥ 453 | 现货 | ||
25 mg | ¥ 757 | 现货 | ||
50 mg | ¥ 1,190 | 现货 | ||
100 mg | ¥ 1,850 | 现货 | ||
500 mg | ¥ 4,580 | 现货 | ||
1 g | ¥ 6,560 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 378 | 现货 |
产品描述 | Efavirenz (DMP 266) is a Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor. The mechanism of action of efavirenz is as a Non-Nucleoside Reverse Transcriptase Inhibitor, and Cytochrome P450 3A Inducer, and Cytochrome P450 2B6 Inducer, and Cytochrome P450 2C9 Inhibitor, and Cytochrome P450 2C19 Inhibitor, and Cytochrome P450 3A4 Inhibitor. The chemical classification of efavirenz is Non-Nucleoside Analog. |
靶点活性 | HIV-1:2.93 nM (Ki) |
体外活性 | Efavirenz has direct inhibitory effect on the mitochondrial respiratory function of cultured glioblastoma and differentiated neuroblastoma cell lines[2]. ER stress markers, including CHOP and GRP78 expression (both protein and mRNA), phosphorylation of eIF2a, and presence of the spliced form of XBP1 are upregulated. Efavirenz also enhances cytosolic Ca2+ content and induced morphological changes in the ER suggestive of ER stress. This response is greatly attenuated in cells with altered mitochondrial function (Rho). The effects of Efavirenz on the ER, and particularly in regard to the mitochondrial involvement, differs from those elicited by a standard pharmacological ER stressor[3]. |
体内活性 | Efavirenz leads to arterial stiffening but, for the dose and duration tested, did not lead to elevated plaque progression in ApoE(-/-) mice[4]. |
激酶实验 | Recombinant RT enzymes are expressed, purified, and assessed for inhibition by Efavirenz (L-743726). Ki and Kii values are determined for each enzyme tested. The wild-type RT exhibited exclusively noncompetitive inhibition kinetics (data not shown), and, therefore, the Ki and Kii values are identical. Pure noncompetitive inhibition is not assumed for the mutant enzymes, and, hence, the values of both Ki and Kii are obtained from the linear mixed-type inhibition equation. The two- to threefold differences between the Ki and Kii values probably reflect a small contribution of competitive inhibition with the mutant RTs[1]. |
细胞实验 | The OCR(O2 consumption rate) is measured in SH-SY5Y and U-251 mg cells exposed to vehicle, 10 μM efavirenz or 25 μM efavirenz for 1 h. (Only for Reference) |
别名 | EFV, 依非韦伦, DMP 266, 依法韦仑, Sustiva, Stocrin, L-743726 |
分子量 | 315.67 |
分子式 | C14H9ClF3NO2 |
CAS No. | 154598-52-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Methanol: 10 mM
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 63 mg/mL (199.58 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Methanol / DMSO | 1 mM | 3.1679 mL | 15.8393 mL | 31.6787 mL | 79.1966 mL |
5 mM | 0.6336 mL | 3.1679 mL | 6.3357 mL | 15.8393 mL | |
10 mM | 0.3168 mL | 1.5839 mL | 3.1679 mL | 7.9197 mL | |
DMSO | 20 mM | 0.1584 mL | 0.792 mL | 1.5839 mL | 3.9598 mL |
50 mM | 0.0634 mL | 0.3168 mL | 0.6336 mL | 1.5839 mL | |
100 mM | 0.0317 mL | 0.1584 mL | 0.3168 mL | 0.792 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Efavirenz 154598-52-4 Autophagy Microbiology/Virology Proteases/Proteasome Reverse Transcriptase HIV Protease HIV inhibit EFV DMP-266 DMP266 Human immunodeficiency virus 依非韦伦 DMP 266 L743726 L 743726 Inhibitor 依法韦仑 Sustiva Stocrin L-743726 inhibitor