| Identification | Back Directory | [Name]
3-Pyridinecarboxamide, 1,4-dihydro-1-methyl-N-(5-nitro-1,2-benzisothiazol-3-yl)-4-oxo- | [CAS]
1821309-39-0 | [Synonyms]
HIV-1 inhibitor-6
3-Pyridinecarboxamide, 1,4-dihydro-1-methyl-N-(5-nitro-1,2-benzisothiazol-3-yl)-4-oxo- | [Molecular Formula]
C14H10N4O4S | [MOL File]
1821309-39-0.mol | [Molecular Weight]
330.32 |
| Chemical Properties | Back Directory | [Boiling point ]
526.9±50.0 °C(Predicted) | [density ]
1.604±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 3.33 mg/mL (10.08 mM; ultrasonic and warming and heat to 80°C) | [form ]
Solid | [pka]
7.26±0.20(Predicted) | [color ]
Yellow to orange |
| Hazard Information | Back Directory | [Uses]
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to agents targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM[1]. | [Biological Activity]
HIV-1 inhibitor-6 (compound 9), a diheteroarylamide-based compound, is a potent HIV-1 pre-mRNA alternative splicing inhibitor. HIV-1 inhibitor-6 blocks HIV replication. HIV-1 inhibitor-6 is active against wild-type HIV-1IIIB (subtype B, X4-tropic) and HIV-1 97USSN54 (subtype A, R5-tropic) with EC50s of 0.6 μM and 0.9 μM, respectively. HIV-1 inhibitor-6 inhibits HIV strains resistant to drugs targeting HIV reverse transcriptase, protease, integrase, and coreceptor CCR5 with EC50s ranging from 0.9 to 1.5 μM[1]. | [IC 50]
X4 HIV-1 (IIIB): 0.6 μM (EC50); R5 HIV-1: 0.9 μM (EC50) | [References]
[1]. Peter K Cheung, et al. A Parallel Synthesis Approach to the Identification of Novel Diheteroarylamide-Based Compounds Blocking HIV Replication: Potential Inhibitors of HIV-1 Pre-mRNA Alternative Splicing. J Med Chem. 2016 Mar 10;59(5):1869-79. |
|
|