1. Anti-infection
    Cell Cycle/DNA Damage
  2. HBV
    DNA/RNA Synthesis
  3. HBV-IN-4

HBV-IN-4 

Cat. No.: HY-131343 Purity: 99.88%
Handling Instructions

HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies.

For research use only. We do not sell to patients.

HBV-IN-4 Chemical Structure

HBV-IN-4 Chemical Structure

CAS No. : 2305897-84-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 317 In-stock
Estimated Time of Arrival: December 31
5 mg USD 300 In-stock
Estimated Time of Arrival: December 31
10 mg USD 480 In-stock
Estimated Time of Arrival: December 31
25 mg USD 950 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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Based on 1 publication(s) in Google Scholar

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Description

HBV-IN-4, a phthalazinone derivative, is a potent and orally active HBV DNA replication inhibitor with an IC50 of 14 nM. HBV-IN-4 induces the formation of genome-free capsids and has potent anti-HBV potencies[1].

IC50 & Target

IC50: 14 nM (HBV DNA replication)[1]

In Vitro

HBV-IN-4 (compound 19f; 0-1 μM; 8 days) treatment inhibits the various forms (relaxed circular [rc] and single-stranded [ss] HBV DNA) in a dose-dependent manner in HepG2.2.15 cells. HBV-IN-4 treatment could also reduce capsidassociated DNAs dose-dependently. HBV-IN-4 could induce the formation of genome-free capsids, including a phenotype of faster-migrating ones[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

HBV-IN-4 (Compound 19f; 50-150 mg/kg; oral administration; twice a day; for 4 weeks; Balb/c male mice) treatment achieves 2.67 log viral load reduction in AAV-HBV/mouse model[1].
HBV-IN-4 (compound 19f) exhibits favorable drug characteristics with low plasma clearance (CL=4.1 mL/min/kg), excellent drug exposure (AUC0-t=49 744 h•ng/L), T1/2 (2.15 hours) and oral bioavailability (F=60.4%) using 20 mg/kg oral administration in mice. HBV-IN-4 also shows good distribution in liver exposure[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c male mice (8-week-old) injected with a recombinant adenoassociated virus (AAV[1]
Dosage: 50 mg/kg, 150 mg/kg
Administration: Oral administration; twice a day; for 4 weeks
Result: Resulted in a 2.67 log reduction of the HBV DNA viral load during a 4-week treatment.
Molecular Weight

479.89

Formula

C₂₄H₁₉ClFN₅O₃

CAS No.

2305897-84-9

SMILES

N#CC1=CC=C(CN(N=C(C2=CC(Cl)=C(NCC(O)CO)N=C2F)C3=C4C=CC=C3)C4=O)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (208.38 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0838 mL 10.4191 mL 20.8381 mL
5 mM 0.4168 mL 2.0838 mL 4.1676 mL
10 mM 0.2084 mL 1.0419 mL 2.0838 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (5.21 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.21 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

HBV-IN-4HBVDNA/RNA SynthesisHepatitis B virusAnti-HBVpharmacokineticoralbioavailabilitylivercapsidadenoassociatedvirusrcDNAssDNAphthalazinoneInhibitorinhibitorinhibit

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Product Name:
HBV-IN-4
Cat. No.:
HY-131343
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