Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tenofovir exalidex (CMX 157) 是一种非环核苷酸类似物 Tenofovir 的脂质结合物,对野生型和抗逆转录病毒耐药的 HIV 毒株,包括多药核苷/核苷酸类似物耐药病毒,都有活性。Tenofovir exalidex 对人外周血单个核细胞中所有主要的HIV-1和HIV-2亚型以及单核细胞来源的巨噬细胞中所有 HIV-1 菌株具有活性,EC50 范围在 0.2 和 7.2 nM 之间。Tenofovir exalidex 具有口服活性,无明显毒性。Tenofovir exalidex 对 HBV 也有活性。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 283 | 现货 | ||
5 mg | ¥ 668 | 现货 | ||
10 mg | ¥ 925 | 现货 | ||
25 mg | ¥ 1,530 | 现货 | ||
50 mg | ¥ 2,650 | 现货 | ||
100 mg | ¥ 3,960 | 现货 |
产品描述 | Tenofovir exalidex (CMX 157) is a lipid-conjugated acyclic nucleotide analog of Tenofovir, demonstrating efficacy against wild-type and antiretroviral-resistant HIV strains, including those resistant to multiple nucleoside/nucleotide analogs. It effectively inhibits all major HIV-1 and HIV-2 subtypes in fresh human PBMCs, as well as all evaluated HIV-1 strains in monocyte-derived macrophages, displaying EC50 values between 0.2 and 7.2 nM. Oral administration of CMX157 shows no apparent toxicity. Additionally, Tenofovir exalidex exhibits antiviral properties against HBV. |
体外活性 | Tenofovir exalidex is consistently >300-fold more active than Tenofovir against multiple viruses in several different cell systems. Tenofovir exalidex will be effective against MNR mutants, including those that are unresponsive to all currently available NRTIs. Notably, the average EC50 in PBMCs for CMX157 against a panel of 27 wild-type HIV-1 isolates representing group M subtypes A to G and group O was 2.6 nM (range, 0.2 to 7.2 nM)[1]. Tenofovir exalidex exerts its therapeutic actions by inhibiting HBV polymerase-mediated HBV DNA elongation, but there is no known binding of cyclophilins to HBV polymerase nor participation of cyclophilins in DNA elongation. The combinational effect of CRV431 (host-targeting) and Tenofovir exalidex (direct-acting) on HBV DNA production is more consistent with the two compounds acting on distinct steps of the HBV life cycle[3]. |
体内活性 | Tenofovir exalidex (Sprague-Dawley rats) is orally available and has no apparent toxicity when given orally to rats for 7 days at doses of 10, 30, or 100 mg/kg/day[2]. Tenofovir exalidex (5-10 mg/kg; oral gavage; daily for a period of 16 days) decreases liver HBV DNA levels dose-dependently[3]. |
别名 | Tenofovir, HDP-Tenofovir, CMX-157, CMX157, CMX 157 |
分子量 | 569.72 |
分子式 | C28H52N5O5P |
CAS No. | 911208-73-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: Insoluble
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。
Tenofovir exalidex 911208-73-6 Immunology/Inflammation Antiviral Tenofovir HDP-Tenofovir CMX-157 CMX157 CMX 157 Inhibitor inhibitor inhibit