TMC125 is a nonnucleoside reverse transcriptase inhibitor with an EC50 of 1.4 to 4.3 nM for wild-type HIV-1. Additionally, TMC125 is highly potent against a wide range of single-mutant and double-mutant NNRTI-resistant HIV-1 strains, including L100I, K103N, Y181C, and L100I+K103N, at EC50s of 3, 1, 7, and 19 nM, respectively. (1)
TMC125 is believed to have a high barrier to development of resistance in vitro based on multiplicity of infection experiments which confirm a profile distinct from other reverse transcriptase inhibitors. (2)
Technical information:
| Chemical Formula: | C20H15BrN6O | |
| CAS #: | 269055-15-4 | |
| Molecular Weight: | 435.28 | |
| Purity: | > 98% | |
| Appearance: | white | |
| Chemical Name: | 4-((6-amino-5-bromo-2-((4-cyanophenyl)amino)pyrimidin-4-yl)oxy)-3,5-dimethylbenzonitrile | |
| Solubility: | Up to 50 mM in DMSO | |
| Synonyms: | TMC125, TMC-125, Etravirine |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Andries 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), 4680-4686. Pubmed ID: 15561844 |
| 2. | Vingerhoets et al., TMC125 Displays a High Genetic Barrier to the Development of Resistance: Evidence from In Vitro Selection Experiments. J. Virol. 2005, 79(20), 12773-12782. Pubmed ID: 16188980 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
