Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Doravirine 是一种高度特异性的HIV-1非核苷逆转录酶抑制剂,对野生型以及K103N 和Y181C 逆转录酶突变体的IC50值分别为 4.5 nM,5.5 nM 和 6.1 nM。
产品描述 | Doravirine is a non-nucleoside reverse transcriptase inhibitor, used in the treatment of HIV/AIDS. |
靶点活性 | Y181C:31nM, K103N:21nM, wild-type virus:12nM, K103N/Y181C:33 nM |
体外活性 | Doravirine exhibits potent antiviral activity against wild-type virus and K103N, Y181C, and K103N/Y181C mutant viruses, with IC50 value of 12, 21, 31, and 33 nM, respectively. [1]? MK-1439 exhibited similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses).[2] |
体内活性 | Administration of 50 mg doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity (AUC0-∞) and C24 h with no change in Cmax. Midazolam AUC0-∞ is slightly reduced by coadministration of doravirine (geometric mean ratio 0.82, 90% CI 0.70, 0.97). [3] |
激酶实验 | FS-3 substrate is solubilized in assay buffer at 500 μM and frozen at -20°C in single-use aliquots for up to 4 weeks. Recombinant autotaxin is diluted in Tris-buffered saline (140 mM NaCl, 5 mM KCl, 1 mM CaCl2, 1 mM MgCl2, 50 mM Tris, pH 8.0) and incubated with compound in DMSO or DMSO alone (final 1% DMSO) for 15 min at 37°C, and the reaction is started with the addition of FS-3 at a final concentration of 1 μM. The reaction is allowed to proceed at 37°C for 30 min and monitored at 520 nm until the uninhibited control compared with a no-enzyme control gave a Z′≥0.5. IC50s are determined in triplicate by using a four-parameter fit[1]. |
别名 | 多拉维林, 多拉韦林, MK-1439 |
分子量 | 425.75 |
分子式 | C17H11ClF3N5O3 |
CAS No. | 1338225-97-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 30 mg/mL (70.46 mM)
( < 1 mg/mL refers to the product slightly soluble or 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。
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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。
Doravirine 1338225-97-0 Microbiology/Virology Proteases/Proteasome Reverse Transcriptase HIV Protease MK1439 多拉维林 MK 1439 inhibit HIV Human immunodeficiency virus 多拉韦林 Inhibitor MK-1439 inhibitor