NNRT-IN-1
NNRT-IN-1 (compound 8r) is a potent non-nucleoside reverse transcriptase (NNRT) inhibitor featuring significantly anti-resistance efficacy. NNRT-IN-1 inhibits the wild-type HIV-1 and five mutant strains with EC50s in the nanomolar range. NNRT-IN-1 displays favorable pharmacokinetic properties.
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- CAS No.: 2925364-09-4
- Formule: C28H22N6O3
- Masse moléculaire:490.51
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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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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | CC50 |
>40.77 μM
Compound: 8r
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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
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[PMID: 36996328] |
In Vitro
NNRT-IN-1 (compound 8r) inhibits the wild-type HIV-1 (EC50=2.3 nM) and five mutant strains, K103N (EC50=8 nM), E138K (EC50=6 nM), double-digit potency against L100I (EC50=13 nM), Y181C (EC50=29 nM), and Y188L (EC50=52 nM)[1].
NNRT-IN-1 shows no apparent inhibitory effect on CYP1A2, CYP2D6, CYP3A4-T, and CYP3A4-M with IC50 values over 50 μM, and exhibits extremely weak activity toward RPV-sensitive CYP2C9 and CYP2C19 subtypes (IC50=18.5 and 23.6 μM)[1].
NNRT-IN-1 displays very weak inhibition of hERG (IC50>40 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NNRT-IN-1 (5 mg/kg; p.o.) exhibits a half-life of 5.18 h, a MRT of 5.21 h, a Cmax value of 616 ng/mL, and the oral bioavailability (F) of 31.19%[1].
NNRT-IN-1 (p.o.) is well tolerated at a dose of 2 g/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2925364-09-4
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Masse moléculaire 490.51
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Formule C28H22N6O3
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SMILES
CONC(C1=C(N=C(N=C1)NC2=CC=C(C=C2)C#N)OC3=C(C=C(C=C3C)C4=CC=C(C=C4)C#N)C)=O
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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-1 Related Classifications
HY-149928 Related Classifications
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