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269055-15-4

269055-15-4 structure
269055-15-4 structure
Name etravirine
Synonyms Benzonitrile, 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-
etravirine
4-({6-Amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl}oxy)-3,5-dimethylbenzonitrile
tmc 125
Description Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
Related Catalog
In Vitro TMC125 is highly active against wild-type HIV-1 (50% effective concentration [EC50]=1.4 to 4.8 nM) and shows some activity against HIV-2 (EC50=3.5 μM). TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus. TMC125 has activity for 19 viruses with EC50 of < 5 nM[1].
In Vivo Etravirine has a high genetic barrier to the development of resistance. In phase IIb trials in treatment-experienced patients, including those infected with virus resistant to NNRTIs and protease inhibitors (PIs), TMC125 is active against HIV resistant to currently available NNRTIs, with a similar tolerability profile to that of the control group[2].
References

[1]. Andries, K., et al. TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother, 2004. 48(12): p. 468

[2]. Lazzarin, A., et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet, 2007. 370(9581): p. 39-48.
Density 1.6±0.1 g/cm3
Boiling Point 637.4±65.0 °C at 760 mmHg
Melting Point 265ºC (dec.)
Molecular Formula C20H15BrN6O
Molecular Weight 435.277
Flash Point 339.3±34.3 °C
Exact Mass 434.049072
PSA 120.64000
LogP 4.19
Vapour Pressure 0.0±1.9 mmHg at 25°C
Index of Refraction 1.703
Storage condition -20°C Freezer
Hazard Codes Xi
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