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.
For research use only. We do not sell to patients.
- CAS No.: 3035807-39-4
- Formula: C22H24ClF3N4O4
- Molecular Weight:500.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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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CAS No. 3035807-39-4
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Molecular Weight 500.90
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)