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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 2925364-09-4
- Fòrmula: C28H22N6O3
- Peso molecular:490.51
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
Descripciòn
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | CC50 |
>40.77 μM
Compound: 8r
|
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: 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
-
No. CAS 2925364-09-4
-
Peso molecular 490.51
-
Fòrmula C28H22N6O3
-
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NNRT-IN-1 Related Classifications
HY-149928 Related Classifications
Powered by Bioz