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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $44 | In Stock | In Stock | |
| 10 mg | $73 | In Stock | In Stock | |
| 25 mg | $152 | In Stock | In Stock | |
| 50 mg | $228 | In Stock | In Stock | |
| 100 mg | $347 | In Stock | In Stock | |
| 200 mg | $511 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $48 | In Stock | 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]. |
| Synonyms | 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/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 50 mg/mL (114.87 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.59 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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