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。

Doravirine is a non-nucleoside reverse transcriptase inhibitor, used in the treatment of HIV/AIDS.

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]

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]

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].

1338225-97-0

C17H11ClF3N5O3

425.75

多拉韦林;多拉维林;MK-1439

DMSO:30 mg/mL (70.46 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years