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Etravirine (R165335) is a diarylpyrimidine non-nucleoside reverse transcriptase inhibitor. Etravirine is designed to be active against HIV isolates with mutations that confer resistance to the two most commonly prescribed first-generation NNRTIs. It can bind the enzyme reverse transcriptase (RT) in multiple conformations, both for native and mutant RT, thereby blocking the enzymatic activity of RT.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $42 | In Stock | |
5 mg | $68 | In Stock | |
10 mg | $113 | In Stock | |
25 mg | $198 | In Stock | |
50 mg | $293 | In Stock | |
100 mg | $403 | In Stock | |
200 mg | $511 | In Stock | |
1 g | $945 | In Stock | |
1 mL x 10 mM (in DMSO) | $94 | In Stock |
Description | Etravirine (R165335) is a diarylpyrimidine non-nucleoside reverse transcriptase inhibitor. Etravirine is designed to be active against HIV isolates with mutations that confer resistance to the two most commonly prescribed first-generation NNRTIs. It can bind the enzyme reverse transcriptase (RT) in multiple conformations, both for native and mutant RT, thereby blocking the enzymatic activity of RT. |
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. [1] [2] |
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[3]. |
Alias | TMC125, R165335 |
Molecular Weight | 435.28 |
Formula | C20H15BrN6O |
Cas No. | 269055-15-4 |
Smiles | O(C1=NC(NC2=CC=C(C#N)C=C2)=NC(N)=C1Br)C3=C(C)C=C(C#N)C=C3C |
Relative Density. | 1.439 g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 50 mg/mL (114.87 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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