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雷特格韦钾盐  ≥98%

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包装规格：5mg 10mg 50mg in glass bottle
溶解性：溶于DMSO（6 mg/mL 超声)
产品描述：基本信息 产品编号：R10208 产品名称：Raltegravir potassium salt CAS: 871038-72-1   储存条件 粉末 -20℃ 四年     分子式： C20H20FKN6O5 溶于液体 -80℃ 两年 分子量 482.51 -20℃ 一个月 化学名：  potassium 4-((4-fluorobenzyl)carbamoyl)-1-methyl-2-(2-(5-methyl-1,3,4-oxadiazole-2-carboxamido)propan-2-yl)-6-oxo-1,6-dihydropyrimidin-5-olate   Solubility (25°C)   体外 DMSO 96mg/mL (198.95mM) Ethanol 10mg/mL (20.72mM) 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 2.0725mL 10.3625mL 20.7250mL 5mM 0.4145mL 2.0725mL 4.1450mL 10mM 0.2072mL 1.0362mL 2.0725mL 50mM 0.0414mL 0.2072mL 0.4145mL   生物活性 产品描述 一种有效的 integrase 抑制剂，用于研究 HIV 感染。 靶点/IC50 HIV integrase()   体外研究 PFV IN carrying the S217H substitution is 10-fold less susceptible to Raltegravir with IC50 of 900 nM. PFV IN displays 10% ofWT activity and is inhibited by Raltegravir with an IC50 of 200 nM, indicating a appr twofold decrease in susceptibility to theIN strand transfer inhibitor (INSTI) compared with WT IN. S217Q PFV IN is as sensitive to Raltegravir as the WT enzyme.Raltegravir is metabolized by glucuronidation, not hepatically. Raltegravir has potent in vitro activity against HIV-1, with a95% inhibitory concentration of 31±20 nM, in human T lymphoid cell cultures. Raltegravir is also active against HIV-2 whenRaltegravir 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 andshould not be used. Raltegravir exhibits weak inhibitory effects on hepatic cytochrome P450 activity. Raltegravir does notinduce CYP3A4 RNA expression or CYP3A4-dependent testosterone 6-β-hydroxylase activity. Raltegravir cellularpermeativity is reduced in the presence of magnesium and calcium[3]. Raltegravir and related HIV-1 integrase (IN) strandtransfer inhibitors (INSTIs efficiently block viral replication[4]. In acutely infected human lymphoid CD4+T-cell lines MT-4 andCEMx174, SIVmac251 replication is efficiently inhibited by Raltegravir, which shows an EC90 in the low nanomolar range.   体内研究 Raltegravir induces viro-immunological improvement of nonhuman primates with progressing SIVmac251 infection. Onenon-human primate shows an undetectable viral load following Raltegravir monotherapy.   推荐实验方法(仅供参考) 细胞实验:   Cell Assay uman MT-4 cells are infected for 2 hours with the SIVmac251, HIV-1 (IIIB) and HIV-2 (CDC 77618) stocks at a multiplicity ofinfection 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 arange of triplicate raltegravir concentrations (0.0001 μM-1 μM). Untreated infected and mock-infected controls are preparedtoo, in order to allow comparison of the data derived from the different treatments. Viral cytopathogeniciy in MT-4 cells isquantitated by the methyl tetrazolium (MTT) method (MT-4/MTT assay) when extensive cell death in control virus-infectedcell cultures is detectable microscopically as lack of capacity to re-cluster. The capability of MT-4 cells to form clusters afterinfection. Briefly, clusters are disrupted by pipetting; and, after 2 hours of incubation at 37°C, the formation of new clustersis assessed by light microscopy (100× magnification). Cell culture supernatants are collected for HIV-1 p24 and HIV2/SIVmac251 p27 core antigenmeasurement by ELISA. In CEMx174-infected cell cultures, which show a propensity to formsyncytia induced by the virus envelope glycoproteins, syncytia are counted, in blindedfashion, by light microscopy for eachwell at 5 days following infection.
保存条件：-20℃

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