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Antiviral API
- Arenavirus
- Cytomegalovirus (CMV)
- Dengue virus
- Endogenous Metabolite
- Enterovirus (EV)
- Epstein-Barr virus (EBV)
- Filovirus
- Flavivirus
- HCV Protease
- Hepatitis B Virus (HBV)
- Hepatitis C Virus (HCV)
- Herpes simplex Virus (HSV)
- HIF/HIF Prolyl-Hydroxylase
- HIV Integrase
- HIV Protease
- Human immunodeficiency Virus (HIV)
- Human papillomavirus (HPV)
- Influenza Virus
- Nipah virus
- Orthopoxvirus
- Others
- Rabies virus (RABV)
- Respiratory syncytial Virus (RSV)
- Reverse Transcriptases (RTs)
- SARS-CoV
- Tobacco mosaic virus (TMV)
- Vesicular stomatitis virus (VSV)
- Virus Protease
- West Nile virus
- Antiviral intermediates
Rilpivirine
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| Category | Human immunodeficiency Virus (HIV) |
| CAS | 500287-72-9 |
| Description | A novel non-nucleoside reverse transcriptase inhibitor. Rilpivirine seems to be well tolerated with less CNS disturbance than Efavirenz, and has non-teratogenic potential. An anti-HIV agent. |
Product Information
| Synonyms | R 278474; TMC 278; R-278474; R278474; TMC278; TMC-278 |
| IUPAC Name | 4-[[4-[4-[(E)-2-cyanoethenyl]-2,6-dimethylanilino]pyrimidin-2-yl]amino]benzonitrile |
| Molecular Weight | 366.428 |
| Molecular Formula | C22H18N6 |
| Canonical SMILES | CC1=CC(=CC(=C1NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C)C=CC#N |
| InChI | 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+ |
| InChIKey | YIBOMRUWOWDFLG-ONEGZZNKSA-N |
| Boiling Point | 634.1±65.0 °C at 760 mmHg |
| Melting Point | 245°C |
| Flash Point | 337.3±34.3 °C |
| Purity | 98% |
| Density | 1.3±0.1 g/cm3 |
| Solubility | In vitro: 10 mM in DMSO |
| Appearance | Light yellow to yellow (Solid) |
| Storage | Powder: -20°C: 3 years; 4°C: 2 years; In solvent: -80°C: 6 months; -20°C: 1 month |
| Complexity | 607 |
| Exact Mass | 366.15929460 |
| Index Of Refraction | 1.665 |
| In Vitro | Rilpivirine(TMC278) is a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. NNRTIs work by binding to and blocking HIV reverse transcriptase, an HIV enzyme. This prevents HIV from replicating and lowers the amount of HIV in the blood. |
| In Vivo | R278474 (10-160 mg/kg; p.o. for 1 month) does not produce abnormal effects in rat, apart from liver weight increase and species-specific thyroid hypertrophy, both at the higher dose levels. R278474 (i.v.) exhibits elimination half-life ranges from 4.4 h in rat to 31 h in dog, and exposure (AUCinf) amounts to 3.1 μg·h/mL (4 mg/kg) in rat, 8.7 μg·h/mL (1.25 mg/kg) in dog, 1.4 μg·h/mL (1.25 mg/ kg) in monkey, and 44·μg h/mL (1.25 mg/kg) in rabbit. R278474 (p.o.) exhibits half-life ranges between 2.8 h in rat and 39 h in dog, and oral bioavailability of 32% and 31% in rat and dog. |
| PSA | 97.42000 |
| Target | HIV; Reverse Transcriptase |
| Vapor Pressure | 0.0±1.9 mmHg at 25°C |
| XLogP3-AA | 4.5 |
