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Etravirine

Catalog No. T2551 CAS 269055-15-4

Synonyms: 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.

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Etravirine, CAS 269055-15-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 42.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 113.00
25 mg	In stock	$ 198.00
50 mg	In stock	$ 293.00
100 mg	In stock	$ 403.00
200 mg	In stock	$ 511.00
1 g	In stock	$ 945.00
1 mL * 10 mM (in DMSO)	In stock	$ 94.00

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Purity: 99.56%

Purity: 97.61%

Biological Description

Chemical Properties

Storage & Solubility Information

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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 39 mg/mL (89.6 mM)

References and Literature

1. Das K, et al. J Med Chem, 2004, 47(10), 2550-2560. 2. Andries K, et al. Antimicrob Agents Chemother, 2004, 48(12), 4680-4686. 3. Lazzarin A, et al. Lancet, 2007, 370(9581), 39-48. 4. Fical L. Vývoj UHPLC-MS/MS metody pro analýzu vybraných antivirotik v HILIC a RP módu[J]. 2020

Citations

1. Ly T T G, Yun J, Ha J S, et al. Inhibitory Effect of Etravirine, a Non-Nucleoside Reverse Transcriptase Inhibitor, via Anterior Gradient Protein 2 Homolog Degradation against Ovarian Cancer Metastasis. International Journal of Molecular Sciences. 2022, 23(2): 944. 2. Islam S, Rahaman M H, Yu M, et al.Anti-Leukaemic Activity of Rilpivirine Is Mediated by Aurora A Kinase Inhibition.Cancers.2023, 15(4): 1044. 3. Ekiciler A, Chen W L K, Bo Y, et al.Quantitative Cytochrome P450 3A4 Induction Risk Assessment Using Human Hepatocytes Complemented with Pregnane X Receptor-Activating Profiles.Drug Metabolism and Disposition.2023, 51(3): 276-284.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library EMA Approved Drug Library Drug Repurposing Compound Library Target-Focused Phenotypic Screening Library Clinical Compound Library Bioactive Compound Library Orally Active Compound Library Pediatric Drug Library Drug-induced Liver Injury (DILI) Compound Library NO PAINS Compound Library

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Etravirine 269055-15-4 Microbiology/Virology Proteases/Proteasome Reverse Transcriptase HIV Protease TMC125 TMC 125 R 165335 Inhibitor R165335 HIV Human immunodeficiency virus TMC-125 inhibit R-165335 inhibitor

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