Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Raltegravir potassium (MK 0518 potassium salt) 是一种整合酶抑制剂,用于研究 HIV 感染。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 247 | 现货 | ||
10 mg | ¥ 372 | 现货 | ||
25 mg | ¥ 652 | 现货 | ||
50 mg | ¥ 1,080 | 现货 | ||
100 mg | ¥ 1,830 | 现货 | ||
200 mg | ¥ 2,720 | 现货 | ||
500 mg | ¥ 4,380 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 263 | 现货 |
产品描述 | Raltegravir potassium (MK 0518 potassium salt) salt(MK0518 potassium salt) is a potent integrase (IN) inhibitor, used to treat HIV infection. |
体外活性 | PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC50 of 900 nM. PFV IN displays 10% of WT activity and is inhibited by Raltegravir with an IC50 of 200 nM which indicates an appr twofold decrease in susceptibility to the IN strand transfer inhibitor (INSTI) compared with WT IN. S217Q PFV IN is as sensitive to Raltegravir as the WT enzyme[1]. Raltegravir is metabolized by glucuronidation, not hepatically. Raltegravir has potent in vitro activity against HIV-1, with a 95% inhibitory concentration of 31±20 nM, in human T lymphoid cell cultures. Raltegravir is also active against HIV-2 when Raltegravir is tested in CEMx174 cells, with an IC95 of 6 nM. Raltegravir metabolism occurs primarily through glucuronidation. Drugs that are strong inducers of the glucuronidation enzyme, UGT1A1, significantly reduce Raltegravir concentrations and should not be used. Raltegravir exhibits weak inhibitory effects on hepatic cytochrome P450 activity. Raltegravir does not induce CYP3A4 RNA expression or CYP3A4-dependent testosterone 6-β-hydroxylase activity[2]. Raltegravir cellular permeativity is reduced in the presence of magnesium and calcium[3]. Raltegravir and related HIV-1 integrase (IN) strand transfer inhibitors (INSTIs efficiently block viral replication[4]. SIVmac251 replication is efficiently inhibited by Raltegravir, which shows an EC90 in the low nanomolar range in acutely infected human lymphoid CD4+ T-cell lines MT-4 and CEMx174[5]. |
体内活性 | Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. One non-human primate exhibits an undetectable viral load following Raltegravir monotherapy[5]. |
细胞实验 | Human MT-4 cells are infected for 2 hours with the SIVmac251, HIV-1 (IIIB) and HIV-2 (CDC 77618) stocks at a multiplicity of infection of, approximately, 0.1. Cells are then washed three times in phosphate buffered saline, and suspended at 5 × 105/mL in fresh culture medium (to primary cells 50 units/mL of IL-2 are added) in 96-well plates, in the presence or absence of a range of triplicate raltegravir concentrations (0.0001 μM-1 μM). Untreated infected and mock-infected controls are prepared too, in order to allow comparison of the data derived from the different treatments. Viral cytopathogeniciy in MT-4 cells is quantitated by the methyl tetrazolium (MTT) method (MT-4/MTT assay) when extensive cell death in control virus-infected cell cultures is detectable microscopically as lack of capacity to re-cluster. The capability of MT-4 cells to form clusters after infection. Briefly, clusters are disrupted by pipetting; and, after 2 hours of incubation at 37°C, the formation of new clusters is assessed by light microscopy (100× magnification). Cell culture supernatants are collected for HIV-1 p24 and HIV-2/SIVmac251 p27 core antigen measurement by ELISA. In CEMx174-infected cell cultures, which show a propensity to form syncytia induced by the virus envelope glycoproteins, syncytia are counted, in blinded fashion, by light microscopy for each well at 5 days following infection. |
别名 | MK 0518 potassium salt, Raltegravir potassium salt, 雷特格韦钾盐 |
分子量 | 482.51 |
分子式 | C20H20FN6O5·K |
CAS No. | 871038-72-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 87 mg/mL(180.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0725 mL | 10.3625 mL | 20.725 mL | 51.8124 mL |
5 mM | 0.4145 mL | 2.0725 mL | 4.145 mL | 10.3625 mL | |
10 mM | 0.2072 mL | 1.0362 mL | 2.0725 mL | 5.1812 mL | |
20 mM | 0.1036 mL | 0.5181 mL | 1.0362 mL | 2.5906 mL | |
50 mM | 0.0414 mL | 0.2072 mL | 0.4145 mL | 1.0362 mL | |
100 mM | 0.0207 mL | 0.1036 mL | 0.2072 mL | 0.5181 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。
Raltegravir potassium 871038-72-1 Microbiology/Virology Proteases/Proteasome HIV Protease Integrase Raltegravir inhibit HIV Inhibitor MK 0518 MK 0518 potassium salt Human immunodeficiency virus Raltegravir potassium salt MK-0518 MK0518 HIV Integrase 雷特格韦钾盐 MK 0518 potassium inhibitor