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Etravirine

🥰Excellent
Catalog No. T2551Cas No. 269055-15-4
Alias TMC125, R165335

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.

Etravirine

Etravirine

🥰Excellent
Purity: 99.56%
Catalog No. T2551Alias TMC125, R165335Cas No. 269055-15-4
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 SizePriceAvailabilityQuantity
2 mg$42In Stock
5 mg$68In Stock
10 mg$113In Stock
25 mg$198In Stock
50 mg$293In Stock
100 mg$403In Stock
200 mg$511In Stock
1 g$945In Stock
1 mL x 10 mM (in DMSO)$94In Stock
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Purity:99.56%
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Product Introduction

Bioactivity
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].
AliasTMC125, R165335
Chemical Properties
Molecular Weight435.28
FormulaC20H15BrN6O
Cas No.269055-15-4
SmilesO(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 & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.2974 mL11.4869 mL22.9737 mL114.8686 mL
5 mM0.4595 mL2.2974 mL4.5947 mL22.9737 mL
10 mM0.2297 mL1.1487 mL2.2974 mL11.4869 mL
20 mM0.1149 mL0.5743 mL1.1487 mL5.7434 mL
50 mM0.0459 mL0.2297 mL0.4595 mL2.2974 mL
100 mM0.0230 mL0.1149 mL0.2297 mL1.1487 mL

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