多拉维林 T3632

Product Introduction
Bioactivity


英文名: Doravirine

描述: Doravirine (MK-1439) 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。

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].

体外活性: Doravirine 对野生型病毒及K103N、Y181C和K103N/Y181C突变病毒展示出强大的抗病毒活性，其IC50值分别为12、21、31和33 nM。[1] MK-1439 对10种不同HIV-1亚型病毒（共93种病毒）显示出了类似的抗病毒活动。[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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 30 mg/mL (70.46 mM)


关键字: MK1439 | Reverse Transcriptase | inhibit | MK 1439 | HIV | Human immunodeficiency virus | Inhibitor | Doravirine

相关产品: PNU-103017 | Miltefosine | Valproic acid sodium salt | Raltegravir potassium | 3'-Azido-3'-deoxy-5-methylcytidine | Coronalolide methyl ester | Etravirine | PF-3450074 | Rottlerin | Ganoderic acid C1

相关库: FDA-Approved Drug Library | Drug Repurposing Compound Library | Approved Drug Library | ReFRAME Related Library | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compounds Library Max | Inhibitor Library | EMA Approved Drug Library | Bioactive Compound Library | Anti-Infection Compound Library

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