Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MK-2048是HIV 整合酶和INR263K 的抑制剂,IC50分别为2.6 nM 和1.5 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 5,920 | 6-8周 | ||
50 mg | ¥ 7,854 | 6-8周 | ||
100 mg | ¥ 11,781 | 6-8周 | ||
200 mg | ¥ 18,173 | 6-8周 | ||
500 mg | ¥ 27,260 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,997 | 6-8周 |
产品描述 | MK-2048 is a potent inhibitor of integrase (IN) and INR263K with IC50 of 2.6 nM and 1.5 nM, respectively. |
靶点活性 | Integrase (R263K):1.5 nM, Integrase:2.6 nM |
体外活性 | MK-2048 inhibits subtype B and subtype C integrase activities with IC50 of 75 nM and 80 nM, respectively. Disintegration is prevented by high concentrations of MK-2048 to a comparable extent with both subtype B and C enzymes. Mutation at the site of R263K slightly increases integrase susceptibility to MK-2048. G118R translates into a decrease in integrase activity and confers resistance to MK-2048. [2] MK-2048 inhibits S217H intasome with an IC50 of 900 nM. By contrast, MK2048 remains fully active against the N224H intasome with an IC50 of 25 nM. MK2048 displays substantially lower dissociation rates compared with raltegravir, another integrase inhibitor. [3] The subsequent selection of E138K partially restores replication capacity to approximately 13% of wt levels and increased resistance to MK-2048 to approximately 8-fold. MK-2048 is active against viruses resistant to RAL and EVG. Exposure to MK-2048 leads to the selection of G118R as a possible novel resistance mutation after 19 weeks. Continued pressure with MK-2048 subsequently leads to an additional substitution after 29 weeks at position E138K, within the IN gene. Although the G118R mutation alone confers only slight resistance to MK-2048 but not to RAL or EVG, its presence arouses a dramatic reduction in viral replication capacity compared to wild-type NL4-3. E138K both partially restores viral replication capacity and also contributes to increased levels of resistance against MK-2048. [4] |
细胞实验 | A total of 7.5×104 PM1 cells per well are infected with clonal NL4-3 virus containing the integrase mutations G118R, E138K, or G118R and E138K or with wild-type viruses (45 ng p24 virus per well) by spinoculation at 1,200 × g for 2 hours at 37 °C. Cells are washed twice to remove unbound virus and then resuspends in RPMI growth medium alone or containing various concentrations of MK-2048, ranging between 0.0256 nM and 2 μM. Experiments is performed, each in duplicate. Supernatant reverse transcriptase (RT) activity is measured at 72 hours postinfection as an indicator of virus replication. Data are normalized based on uninfected and no-drug controls included in each experiment. Viral replication capacity is determined in PM1 cells using the same methodology as that used to determine EC50s, by comparing levels of supernatant RT activity of each mutant virus to those of wild-type virus in the absence of MK-2048.(Only for Reference) |
别名 | MK2048 |
分子量 | 461.87 |
分子式 | C21H21ClFN5O4 |
CAS No. | 869901-69-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 9 mg/mL (19.48 mM)
H2O: <1 mg/mL
Ethanol: <1 mg/mL
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1651 mL | 10.8256 mL | 21.6511 mL | 54.1278 mL |
5 mM | 0.433 mL | 2.1651 mL | 4.3302 mL | 10.8256 mL | |
10 mM | 0.2165 mL | 1.0826 mL | 2.1651 mL | 5.4128 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。
MK-2048 869901-69-9 Microbiology/Virology Proteases/Proteasome HIV Protease Integrase HIV Human immunodeficiency virus inhibit MK2048 Inhibitor HIV Integrase MK 2048 inhibitor