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Etravirine

SKU: orb1305326

Description

Etravirine (R165335) is a second-generation diarylpyrimidine NNRTI effective against HIV strains resistant to first-generation NNRTIs. It inhibits reverse transcriptase by binding in multiple conformations. This compound is utilized in antiviral research for both in vitro enzymatic assays and in vivo studies of HIV infection and drug resistance.

Research Area

Infectious Disease & Virology, Protein Biochemistry

Images & Validation

Key Properties

CAS Number269055-15-4
MW435.28
Purity99.74%
FormulaC20H15BrN6O
SMILESO(C1=NC(NC2=CC=C(C#N)C=C2)=NC(N)=C1Br)C3=C(C)C=C(C#N)C=C3C
TargetHIV Protease,Reverse Transcriptase
SolubilityDMSO:250 mg/mL (574.34 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.59 mM)

Bioactivity

In Vivo
Etravirine (TMC125) demonstrates a high genetic barrier against resistance development and remains effective against HIV strains resistant to existing non-nucleoside reverse transcriptase inhibitors (NNRTIs), including those also resistant to protease inhibitors (PIs). Its tolerability profile, assessed in phase IIb trials with treatment-experienced patients, is comparable to the control group.
In Vitro
Etravirine (TMC125), is highly active against wild-type HIV-1 with EC50 of 1.4 nM to 4.8 nM and shows some activity against HIV-2 with EC50 of 3.5 μM. TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Inhibitor, Human immunodeficiency virus, HIVProtease, HIV, HIV Protease, Etravirine, inhibit, ReverseTranscriptase, Reverse Transcriptase, TMC 125, TMC125, TMC-125, R165335, R-165335, R 165335

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Key Properties

No computed properties available.

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Etravirine (orb1305326)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

2 mg
$ 70.00
1 ml x 10 mM (in DMSO)
$ 90.00
5 mg
$ 90.00
10 mg
$ 120.00
25 mg
$ 200.00
50 mg
$ 290.00
100 mg
$ 410.00
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