R 82913
R 82913 Basic information
- Product Name:
- R 82913
- Synonyms:
-
- R 82913
- [5S,(+)]-4,5,6,7-Tetrahydro-9-chloro-5-methyl-6-(3-methyl-2-butenyl)imidazo[4,5,1-jk][1,4]benzodiazepine-2(1H)-thione
- 4,5,6,7-Tetrahydro-5α-methyl-6-(3-methyl-2-butenyl)-9-chloroimidazo[4,5,1-jk][1,4]benzodiazepine-2(1H)-thione
- 9-Chloro TIBO
- TIBO-R82913
- TIBO-R-82913
- (+)-(S)-4,5,6,7-tetrahydro-9-chloro-5-methyl-6-(3-methyl-2-butenyl)imidazo<4,5,1-jk><1,4>benzodiazepine-2(1H)-thione
- 9-Cl-Tibo
- CAS:
- 126347-69-1
- MF:
- C16H20ClN3S
- MW:
- 321.87
- Mol File:
- 126347-69-1.mol
R 82913 Chemical Properties
- Boiling point:
- 429.7±55.0 °C(Predicted)
- Density
- 1.30±0.1 g/cm3(Predicted)
- pka
- 11.35±0.40(Predicted)
R 82913 Usage And Synthesis
Uses
R82913 (9-Cl-TIBO) is a potent and high selective inhibitor of HIV-1 reverse transcriptase with antiviral activity on both an RNA template (negative strand synthesis) and a DNA template (positive strand synthesis). R82913 inhibits the replication of different strains of HIV-I in CEM cells with a median IC50 value of of 0.15 μM[1][2].
References
[1] White EL, et al. A TIBO derivative, R82913, is a potent inhibitor of HIV-1 reverse transcriptase with heteropolymer templates. Antiviral Res. 1991 Oct;16(3):257-66. DOI:10.1016/0166-3542(91)90005-c
[2] Larder BA. 3'-Azido-3'-deoxythymidine resistance suppressed by a mutation conferring human immunodeficiency virus type 1 resistance to nonnucleoside reverse transcriptase inhibitors. Antimicrob Agents Chemother. 1992 Dec;36(12):2664-9. DOI:10.1128/AAC.36.12.2664