NNRT-IN-4
NNRT-IN-4 (Compound 10p) is an inhibitor for non-nucleoside reverse transcriptase (NNRT) with an IC50 of 0.713 µM for HIV-1 RT. NNRT-IN-4 exhibits antiviral efficacy, inhibits HIV-1 wildtype and mutant strains with EC50 of 6-63 nM. NNRT-IN-4 exhibits a slight inhibitory activities against hERG (IC50=25.9 µM) and CYP enzymes (IC50>50 µM). NNRT-IN-4 exhibits good tolerability and safety in mice (2 g/kg).
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- Formule: C36H38N6O4
- Masse moléculaire:618.72
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | CC50 |
>202.17 μM
Compound: 10p
|
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
|
[PMID: 38996652] |
Chemical Information
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Masse moléculaire 618.72
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Formule C36H38N6O4
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SMILES
CC1=C(OC2=C(C(OCC)=O)C=NC(NC3CCN(CC4=CC=C(C(NC)=O)C=C4)CC3)=N2)C(C)=CC(C5=CC=C(C#N)C=C5)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Huang WJ, et al., Structure-based discovery of novel piperidine-biphenyl-DAPY derivatives as non-nucleoside reverse transcriptase inhibitors featuring improved potency, safety, and selectivity: From piperazine-biphenyl-DAPYs to piperidine-biphenyl-DAPYs. Eur J Med Chem. 2024 Jul 10;276:116668. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)