2. Anti-infection
  3. HCV
  4. 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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HCV-IN-38

HCV-IN-38 Chemical Structure

CAS No. : 3035807-39-4

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HCV-IN-38 Related Antibodies

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Description

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[1].

IC50 & Target

EC50: 15 nM (HCV) in Huh7.5 cells[1]
Cellular Effect
Cell Line Type Value Description References
Huh-7.5 CC50
6.47 μM
Compound: 80
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
[PMID: 34883293]
Huh-7.5 CC50
6470 nM
Compound: 8e
Cytotoxicity against human Huh7.5 cells
Cytotoxicity against human Huh7.5 cells
[PMID: 38061229]
NCI-H460 CC50
19.21 μM
Compound: 8e
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
[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.

HCV-IN-38 Related Antibodies

Cell Cytotoxicity Assay

Cell Line: Huh7.5 cells[1]
Concentration: 0-20 μM
Incubation Time: 72 hours
Result: Exhibited low cytotoxicity with CC50=6.47 μM.
In Vivo

HCV-IN-38 (2 μM; 4 hours) has decent plasma stability (t1/2, rat=16.9 h and t1/2, human=19.9 h)[1].
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.

Animal Model: SD rats (180-220 g, n=3)[1]
Dosage: 2 or 10 mg/kg
Administration: i.v. and p.o., single (Pharmacokinetic Analysis)
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%.
Animal Model: Kunming mice (n=6)[1]
Dosage: 50, 100, 150, and 200 mg/kg
Administration: i.p., single
Result: Demonstrated modest safety profiles with LD50 values higher than 150 mg/kg.
Molecular Weight

500.90

Formula

C22H24ClF3N4O4
CAS No.
SMILES

CN(C1CN(C1)CC2=CC=C(C=C2C(F)(F)F)NC(C3=CC=C(C([N+]([O-])=O)=C3)OCCCl)=O)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HCV-IN-38 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HCV-IN-383035807-39-4HCVHepatitis C virusBiaryl amideOralSelectivityHuh7.5 cellsSD ratsInhibitorinhibitorinhibit

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