[CAS NO. 1338225-97-0]  Doravirine (MK-1439)

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PRODUCTS SPECIFICATIONS [1338225-97-0]

Catelog
SLK-S6492
Brand
Selleck
CAS
1338225-97-0

DESCRIPTION [1338225-97-0]

Overview

MDLMFCD22417167
Molecular Weight425.75
Molecular FormulaC17H11C1F3N5O3
SMILESO(C1=C(C(F)(F)F)C=CN(CC=2N(C)C(=O)NN2)C1=O)C3=CC(C#N)=CC(Cl)=C3

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.3488 mL11.7440 mL23.4880 mL
5 mM0.4698 mL2.3488 mL4.6976 mL
10 mM0.2349 mL1.1744 mL2.3488 mL
50 mM0.0470 mL0.2349 mL0.4698 mL

Description

Doravirine (MK-1439) is a novel inhibitor with IC50 values of 12, 9.7, and 9.7 nM against the wild type (WT) and K103N and Y181C reverse transcriptase (RT) mutants, respectively, in a biochemical assay. It is highly specific with minimum off-target activities.

In vitro

MK-1439 exhibits greater than 10,000-fold selectivity with respect to the cellular DNA polymerases α, ß, and γ with IC50s of >100 μM. In the screen with more than 110 protein targets including enzymes, transporters, ion channels, and receptor, MK-1439 shows an IC50 of greater than 10 μM against all targets except 5-HT2ß, where an IC50 of 2.5 μM is noted in a ligand binding assay. However, the 5-HT2ß activity is not observed in a functional cell-based assay monitoring the accumulation of inositol-1-phosphate. Therefore, the binding activity does not appear to translate into a 5-HT2ß functional response. MK-1439 does not display cytotoxicity in activated CD4+ T cells, PBMCs, monocytes, macrophages proliferating transformed cell lines, such as MT4, SupT1, and HL60 cell lines at concentrations of up to 100 μM.


Synonyms

Benzonitrile, 3-chloro-5-[[1-[(4,5-dihydro-4-methyl-5-oxo-1H-1,2,4-triazol-3-yl)methyl]-1,2-dihydro-2-oxo-4-(trifluoromethyl)-3-pyridinyl]oxy]-
3-Chloro-5-[[1-[(4,5-dihydro-4-methyl-5-oxo-1H-1,2,4-triazol-3-yl)methyl]-1,2-dihydro-2-oxo-4-(trifluoromethyl)-3-pyridinyl]oxy]benzonitrile
MK 1439
Doravirine
3-Chloro-5-[1-[(4-methyl-5-oxo-1H-1,2,4-triazol-3-yl)methyl]-2-oxo-4-(trifluoromethyl)pyridin-3-yl]oxybenzonitrile
Pifeltro