Molecular Weight(MW): 425.75
Doravirine is a novel HIV-1 nonnucleoside reverse transcriptase 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.
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Choose Selective Reverse Transcriptase Inhibitors
|Description||Doravirine is a novel HIV-1 nonnucleoside reverse transcriptase 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.|
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.
In rats dosed IV at 1 mpk (60%PEG200), the clearance (CL) of MK-1439 is 5.4 mL/min/kg and the half time is 4.4 hr. Its volume of distribution (Vd) is 2.3 L/kg. The oral bioavailability of MK-1439 is 57% (doesed PO at 5 mpk). In dogs dosed IV at 0.5 mpk, the CL of MK-1439 is 0.36 mL/min/kg and half-time is 37 hr. The oral bioavailability of MK-1439 is 52% (doesed PO at 1 mpk). Overall, The pharmacokinetic profile of MK-1439 in preclinical species is favorable.
|In vitro||DMSO||85 mg/mL (199.64 mM)|
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