| CAS NO: | 500287-72-9 |
| 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) | 366.42 |
|---|---|
| Formula | C22H18N6 |
| CAS No. | 500287-72-9 (free base); |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 73 mg/mL (199.2 mM) |
| Water:<1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Other info | Chemical Name: 4-{[4-({4-[(E)-2-cyanovinyl]-2,6-dimethylphenyl}amino)pyrimidin-2-yl]amino}benzonitrile InChi Key: YIBOMRUWOWDFLG-ONEGZZNKSA-N InChi Code: InChI=1S/C22H18N6/c1-15-12-18(4-3-10-23)13-16(2)21(15)27-20-9-11-25-22(28-20)26-19-7-5-17(14-24)6-8-19/h3-9,11-13H,1-2H3,(H2,25,26,27,28)/b4-3+ SMILES Code: N#CC1=CC=C(NC2=NC=CC(NC3=C(C)C=C(/C=C/C#N)C=C3C)=N2)C=C1 |
| Synonyms | R-278474, DB08864, TMC278; R 278474, D08864, TMC-278; R278474, D08864, TMC 278; Rilpivirine; Rekambys; Cabenuva; Edurant. |
| In Vitro | In vitro activity: Rilpivirine shows antiviral activity with EC50 ranging from 0.1 nM to 2 nM against wild-type and selected site-directed single and double mutants of HIV-1. Rilpivirine inhibits viral replication at concentrations at which first-generation NNRTIs could not suppress replication, and produces a high genetic barrier to resistance development. |
|---|---|
| In Vivo | After iv administration of Rilpivirine, Elimination half-life ranges from 4.4 h in rat to 31 h in dog. After oral administration of Rilpivirine in PEG 400, half-life ranges between 2.8 h in rat and 39 h in dog. |
| Animal model | Sprague–Dawley rat, beagle dog, white New Zealand rabbit, and cynomolgus monkey. |
| Formulation & Dosage | Dissolved in PEG 400; 4 mg/kg ( rat); 1.25 mg/kg (other species); i.v. or p.o. |
| References | J Med Chem. 2005 Mar 24;48(6):1901-9; Antimicrob Agents Chemother. 2010 Feb;54(2):718-27. |
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