| Identification | Back Directory | [Name]
[1,1'-Biphenyl]-4-carbonitrile, 4'-[(S)-[2-[(4-cyanophenyl)amino]-4-pyrimidinyl]hydroxymethyl]-3'-methoxy- | [CAS]
2475658-75-2 | [Synonyms]
HIV-1 inhibitor-24
1,1'-Biphenyl]-4-carbonitrile, 4'-[(S)-[2-[(4-cyanophenyl)amino]-4-pyrimidinyl]hydroxymethyl]-3'-methoxy-
[1,1'-Biphenyl]-4-carbonitrile, 4'-[(S)-[2-[(4-cyanophenyl)amino]-4-pyrimidinyl]hydroxymethyl]-3'-methoxy- | [Molecular Formula]
C26H19N5O2 | [MOL File]
2475658-75-2.mol | [Molecular Weight]
433.46 |
| Hazard Information | Back Directory | [Uses]
HIV-1 inhibitor-24 (compound S-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 9.5 nM. HIV-1 inhibitor-24 has high antiretroviral activity against WT HIV-1 with an EC50 of 1.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 9.07 μM in MT-4 cells. HIV-1 inhibitor-24 is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety[1]. | [in vivo]
HIV-1 inhibitor-24 (2 g/kg; IG; single dosage) is well tolerated at a dose of 2 g/kg in mice and has a significant cardiovascular safety[1]. | Animal Model: | Mice[1] | | Dosage: | 2 g/kg | | Administration: | IG; single dosage | | Result: | Exhibited well tolerance at a dose of 2 g/kg in mice and a significant cardiovascular safety. |
| [IC 50]
HIV-1 (WT): 1.6 nM (EC50) | [References]
[1] Chen X, et al. Bioisosterism-based design and enantiomeric profiling of chiral hydroxyl-substituted biphenyl-diarylpyrimidine nonnucleoside HIV-1 reverse transcriptase inhibitors. Eur J Med Chem. 2020;202:112549. DOI:10.1016/j.ejmech.2020.112549 |
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