Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Doravirine (MK-1439) is a non-nucleoside reverse transcriptase inhibitor, used in the treatment of HIV/AIDS.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 45.00 | |
2 mg | In stock | $ 63.00 | |
5 mg | In stock | $ 98.00 | |
10 mg | In stock | $ 178.00 | |
25 mg | In stock | $ 353.00 | |
50 mg | In stock | $ 547.00 | |
100 mg | In stock | $ 789.00 | |
500 mg | In stock | $ 1,630.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 133.00 |
Description | Doravirine (MK-1439) is a non-nucleoside reverse transcriptase inhibitor, used in the treatment of HIV/AIDS. |
Targets&IC50 | Y181C:31nM, K103N:21nM, Virus (WT):12nM, K103N/Y181C:33 nM |
In vitro | 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] |
In vivo | 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] |
Kinase Assay | 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]. |
Synonyms | MK-1439 |
Molecular Weight | 425.75 |
Formula | C17H11ClF3N5O3 |
CAS No. | 1338225-97-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30 mg/mL (70.46 mM)
You can also refer to dose conversion for different animals. More
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Doravirine 1338225-97-0 Microbiology/Virology Proteases/Proteasome HIV Protease Reverse Transcriptase MK1439 inhibit MK 1439 HIV Human immunodeficiency virus Inhibitor MK-1439 inhibitor