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Purity: ≥98%
Etravirine (formerly TMC-125; R-165335) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV. It was also approved in 2008. Etravirine, in combination with other anti-retrovirals, is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in antiretroviral treatment-experienced adult patients, who have evidence of viral replication and HIV-1 strains resistant to a NNRTI and other antiretroviral agents.
| ln Vitro |
TMC125 exhibits significant efficacy against HIV-2 (EC50=3.5 μM) and wild-type HIV-1 (50% effective concentration [EC50]=1.4 to 4.8 nM). A number of HIV-1 group M subtypes, circulating recombinant forms, and a group O virus are also inhibited by TMC125. 19 viruses had TMC125 activity with an EC50 of less than 5 nM[1].
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| ln Vivo |
The development of resistance to etravirine is very genetically resistant. TMC125 has demonstrated activity against HIV resistance to currently available NNRTIs in phase IIb trials involving treatment-experienced individuals, including those infected with virus resistant to NNRTIs and protease inhibitors (PIs), while maintaining a tolerability profile comparable to the control group[2].
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| References |
[1]. Andries, K., et al. TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother, 2004. 48(12): p. 468
[2]. Lazzarin, A., et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet, 2007. 370(9581): p. 39-48. |
| Molecular Formula |
C20H15BRN6O
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| Molecular Weight |
435.28
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| CAS # |
269055-15-4
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| Related CAS # |
Etravirine-d4;1142095-93-9;Etravirine-d8;1142096-06-7
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| SMILES |
N#CC1=CC(C)=C(C(C)=C1)OC2=NC(NC3=CC=C(C=C3)C#N)=NC(N)=C2Br
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| InChi Key |
PYGWGZALEOIKDF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H15BrN6O/c1-11-7-14(10-23)8-12(2)17(11)28-19-16(21)18(24)26-20(27-19)25-15-5-3-13(9-22)4-6-15/h3-8H,1-2H3,(H3,24,25,26,27)
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| Chemical Name |
4-(6-Amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yloxy)-3,5-dimethylbenzonitrile
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.74 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2974 mL | 11.4869 mL | 22.9737 mL | |
| 5 mM | 0.4595 mL | 2.2974 mL | 4.5947 mL | |
| 10 mM | 0.2297 mL | 1.1487 mL | 2.2974 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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