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.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
EC50: 15 nM (HCV) in Huh7.5 cells[1]
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HCV-IN-38 Related Classifications
HY-115989 Related Classifications
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