269055-15-4
Etravirine
CAS: 269055-15-4;394729-17-0
Molecular Formula: C20H15BrN6O
269055-15-4 - Names and Identifiers
269055-15-4 - Physico-chemical Properties
| Molecular Formula | C20H15BrN6O |
| Density | 1.439 g/cm3 |
| Melting Point | .265°C (dec.) |
| Boling Point | 637.4±65.0 °C(Predicted) |
| Flash Point | 339.3°C |
| Solubility | DMSO 42 mg/mL Water <1 mg/mL Ethanol <1 mg/mL |
| Vapor Presure | 3.82E-16mmHg at 25°C |
| Appearance | White to off-white solid |
| Color | White to Off-White |
| pKa | 1.23±0.10(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| Sensitive | Sensitive to heat and light |
| Refractive Index | 1.702 |
| In vitro study | Etravirine (TMC125), is high 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 inhibit a series of HIV-1 group M subtypes and circular combined forms and a group O virus. Etravirine (TMC125) was highly effective against wild-type HIV-1, with an EC50 of 1.4 nM to 4.8 nM, and showed some activity against HIV-2, with an EC50 of 3.5 μm. TMC125 also inhibits a series of HIV-1 M-type subunits and circulating recombinant forms as well as O-type Virus. |
| In vivo study | Etravirine has a high genetic barrier to the development of resistance. In phase IIb trials in treatment-experienced patients, included with virus resistant to NNRTIs and protein inhibitors (PIs), TMC125 is active against HIV resistant to current available NNRTIs, with a similar tolerance profile to that of the control group. Etravirine has a high genetic barrier to resistance development. In the Phase IIb trial, TMC125 was active against existing NNRTIs-resistant HIV in multiple-treated patients, including those infected with NNRTIs-resistant and protease inhibitor-resistant (PIs) Virus, similar tolerability to the control group. |
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