HCV-IN-38
HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile.
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- No. CAS: 3035807-39-4
- Fòrmula: C22H24ClF3N4O4
- Peso molecular:500.90
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Almacenamiento:
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Actividad biológica
EC50: 15 nM (HCV) in Huh7.5 cells[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7.5 | CC50 |
6.47 μM
Compound: 80
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Cytotoxicity against human Huh7.5 cells assessed as inhibition of cell growth measured after 96 hrs by MTT assay
Cytotoxicity against human Huh7.5 cells assessed as inhibition of cell growth measured after 96 hrs by MTT assay
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[PMID: 34883293] |
| Huh-7.5 | CC50 |
6470 nM
Compound: 8e
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Cytotoxicity against human Huh7.5 cells
Cytotoxicity against human Huh7.5 cells
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[PMID: 38061229] |
| NCI-H460 | CC50 |
19.21 μM
Compound: 8e
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Cytotoxicity against human NCI-H460 cells incubated for 72 hrs by CCK-8 assay
Cytotoxicity against human NCI-H460 cells incubated for 72 hrs by CCK-8 assay
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[PMID: 38061229] |
HCV-IN-38 (compound 80) (0-20 μM; 72 hours) exhibits high anti-HCV activity with EC50=15 nM and low cytotoxicity with CC50=6.47 μM in Huh7.5 cells[1].
HCV-IN-38 (2 μM; 2 hours) has moderate permeability (0.5 < Papp < 2.5 (×10-6 cm/s))[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Huh7.5 cells[1]
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Concentration:0-20 μM
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Incubation Time:72 hours
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Result:Exhibited low cytotoxicity with CC50=6.47 μM.
HCV-IN-38 (2 mg/kg for i.p., 10 mg/kg for p.o., single) exhibits satisfying PK properties with an oral total exposure (AUC) of 1502 ng h/mL, medium in vivo clearance (38.3 mL/min/kg), Cmax of 452 ng/mL, and moderate bioavailability of 34%[1].
HCV-IN-38 (50-200 mg/kg; i.p., single) has modest safety profiles with LD50 values higher than 150 mg/kg[1].
Pharmacokinetic Parameters of HCV-IN-38 in Sprague-Dawley rats[1].
| IV (2 mg/kg) | PO (10 mg/kg) | |
| AUC0-last (ng·h/mL) | 889 ± 179 | 1502 ± 342 |
| AUC0-inf (ng·h/mL) | 898 ± 184 | 1525 ± 360 |
| MRT0-last (h) | 1.36 ± 0.182 | 2.95 ± 0.276 |
| MRT0-inf (h) | 1.45 ± 0.211 | 3.10 ± 0.290 |
| Cmax (ng/mL) | 452 ± 149 | |
| T1/2 (h) | 1.24 ± 0.101 | 1.90 ± 0.492 |
| Tlast (h) | 8.00 | 12.0 |
| Tmax (h) | 1.00 | |
| Vdss (L/kg) | 3.26 ± 0.426 | |
| Cl (mL/min/kg) | 38.3 ± 8.89 | |
| F (%) | 34 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD rats (180-220 g, n=3)[1]
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Dosage:2 or 10 mg/kg
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Administration:i.v. and p.o., single (Pharmacokinetic Analysis)
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Result:Exhibited satisfying PK properties with an oral total exposure (AUC) of 1502 ng h/mL, medium in vivo clearance (38.3 mL/min/kg), Cmax of 452 ng/mL, and moderate bioavailability of 34%.
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Animal Model:Kunming mice (n=6)[1]
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Dosage:50, 100, 150, and 200 mg/kg
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Administration:i.p., single
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Result:Demonstrated modest safety profiles with LD50 values higher than 150 mg/kg.
Chemical Information
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No. CAS 3035807-39-4
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Peso molecular 500.90
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Fòrmula C22H24ClF3N4O4
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SMILES
CN(C1CN(C1)CC2=CC=C(C=C2C(F)(F)F)NC(C3=CC=C(C([N+]([O-])=O)=C3)OCCCl)=O)C
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Envío
Room temperature in continental US; may vary elsewhere.
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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)
HCV-IN-38 Related Classifications
HY-115989 Related Classifications
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