| Description | Rilpivirine (R278474) is a diarylpyrimidine derivative and reverse transcriptase inhibitor with antiviral activity against HIV-1 that is used in the treatment of HIV infections. |
| In vitro | 溶解在PEG 400中的Rilpivirine,静脉注射在大鼠中( 4 mg/kg),在犬中（1.25 mg/kg）,半衰期分别为4.4小时和31小时. |
| In vivo | 在野生型和选择性定点单一和双重HIV-1突变体中（EC50=0.1-2 nM）,Rilpivirine具有抗病毒活性。 |
| Synonyms | TMC278, R278474, 利匹韦林, DB08864 |
| molecular weight | 366.42 |
| Molecular formula | C22H18N6 |
| CAS | 500287-72-9 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 55 mg/mL (150.1 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Janssen PA, et al. J Med Chem. 2005, 48(6), 1901-1909. 2. Azijn H, et al. Antimicrob Agents Chemother. 2010, 54(2), 718-727. 3. Fical L. Vývoj UHPLC-MS/MS metody pro analýzu vybraných antivirotik v HILIC a RP módu[J]. 2020 4. Kang D, Pang X, Lian W, et al. Discovery of VEGFR2 inhibitors by integrating naïve Bayesian classification, molecular docking and drug screening approaches[J]. RSC Advances. 2018 Jan 8(10): 5286-5297. 5. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes[J]. Molecules. 2021, 26(8): 2123. |
| Citations | 1. Bao H, Yan J, Huang J, et al.Activation of endogenous retrovirus triggers microglial immuno-inflammation and contributes to negative emotional behaviors in mice with chronic stress.Journal of Neuroinflammation.2023, 20(1): 1-16. 2. Liu K, Hao Z, Zheng H, et al.Repurposing of rilpivirine for preventing platelet β3 integrin-dependent thrombosis by targeting c-Src active autophosphorylation.Thrombosis Research.2023 3. Islam S, Rahaman M H, Yu M, et al.Anti-Leukaemic Activity of Rilpivirine Is Mediated by Aurora A Kinase Inhibition.Cancers.2023, 15(4): 1044. 4. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes. Molecules. 2021, 26(8): 2123. 5. Kang D, Pang X, Lian W, et al. Discovery of VEGFR2 inhibitors by integrating naïve Bayesian classification, molecular docking and drug screening approaches. RSC Advances. 2018 Jan 8(10): 5286-5297. |