| CAS NO: | 269055-15-4 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 435.28 |
|---|---|
| Formula | C20H15BrN6O |
| CAS No. | 269055-15-4 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 42 mg/mL (96.5 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Other info | Chemical Name: 4-(6-Amino-5-bromo-2-(4-cyanoanilino)pyrimidin-4-yloxy)-3,5-dimethylbenzonitrile InChi Key: PYGWGZALEOIKDF-UHFFFAOYSA-N 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) SMILES Code: N#CC1=CC(C)=C(OC2=NC(NC3=CC=C(C#N)C=C3)=NC(N)=C2Br)C(C)=C1 |
| Synonyms | R-165335; TMC-125; R165335; TMC125; R 165335; TMC 125; R165335; Etravirine. Intelence. |
| In Vitro | In vitro activity: 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. |
|---|---|
| In Vivo | Etravirine has a high genetic barrier to the development of resistance. In phase IIb trials in treatment-experienced patients, including those infected with virus resistant to NNRTIs and protease inhibitors (PIs), TMC125 is active against HIV resistant to currently available NNRTIs, with a similar tolerability profile to that of the control group. |
| Animal model | NA |
| Formulation & Dosage | NA |
| References | J Med Chem. 2004 May 6;47(10):2550-60; Antimicrob Agents Chemother. 2004 Dec;48(12):4680-6; Lancet. 2007 Jul 7;370(9581):39-48. |
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