NNRT-IN-10
NNRT-IN-10 is a potent, selective and orally active non-nucleoside HIV-1 reverse transcriptase (NNRTI) inhibitor with with an EC50 values ranging from 1.16 to 18.3 nM for HIV and its mutant strains. NNRT-IN-10 exhibits good pharmacokinetic properties and favorable safety profiles. NNRT-IN-10 can be used for the study of AIDS, caused by HIV-1.
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- CAS No.: 2459751-62-1
- Formule: C31H32N6O3S
- Masse moléculaire:568.69
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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HIV-1 (WT) 1.16 nM (EC50) |
CYP1A2 56.6 μM (IC50) |
CYP2C9 6.76 μM (IC50) |
CYP2C19 8.47 μM (IC50) |
CYP2D6 12.7 μM (IC50) |
NNRT-IN-10 (48 h) (Compound 5i3) with improved resistance profiles and no apparent cytotoxicity, with EC50 values of 1.16 nM (HIV-1, WT), 2.64 nM (P1579), 12.5 nM (P5375), 3.70 nM (P1833) and 18.3 (P5735), and EC50 = 11.1 nM for the Rilpivirine (HY-10574)-resistant strain GH9, respectively in TZM-bl cells[1]. NNRT-IN-10 (5 days) suppresses the replication of HIV-1 IIIB very effectively at single-digit nanomolar levels (EC50 = 1.4 nM) in MT-4 cells[1]. NNRT-IN-10 shows only faint inhibition of CYP1A2 (IC50 = 56.6 μM), CYP2C9 (IC50 = 6.76 μM), CYP2C19 (IC50 = 8.47 μM), and CYP2D6 (IC50 = 12.7 μM)[1]. NNRT-IN-10(24 h) displays potassium channel inhibitory activity with an IC50 value of 1.48 μM in CHO-hERG cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | T1/2 | AUC0-inf | AUC0-last | Vd | MRT0-last | MRT0-inf | F | Tmax | Cmax |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat | 2 mg/kg | i.v. | 20.6 mL/min/kg | 1.59 h | 1675 ng·h/mL | 1661 ng·h/mL | 1513 mL/kg | 1.17 h | 1.25 h | / | / | / |
| Rat | 20 mg/kg | p.o. | / | 1.77 h | 10033 ng·h/mL | 9934 ng·h/mL | / | 3.37 h | 3.48 h | 59.9 % | 0.417 h | 2354 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2459751-62-1
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Masse moléculaire 568.69
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Formule C31H32N6O3S
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SMILES
CC1=CC(/C=C/C#N)=CC(C)=C1OC2=C(C=CC=N3)C3=NC(NC4CCN(CC5=CC=C(S(C)(=O)=O)C=C5)CC4)=N2
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NNRT-IN-10 Related Classifications
HY-174417 Related Classifications
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