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

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.

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HBV-IN-4 Chemical Structure

HBV-IN-4 Chemical Structure

CAS No. : 2305897-84-9

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Customer Review

Based on 1 publication(s) in Google Scholar

HBV-IN-4 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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]
Cellular Effect
Cell Line Type Value Description References
HepG2 2.2.15 CC50
> 100 μM
Compound: 19f
Cytotoxicity in human HepG2.2.15 cells assessed as reduction in cell viability incubated for 8 days by MTT assay
Cytotoxicity in human HepG2.2.15 cells assessed as reduction in cell viability incubated for 8 days by MTT assay
[PMID: 32692159]
HepG2 2.2.15 IC50
0.014 μM
Compound: 19f
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic HBV-DNA replication incubated for 8 days by real-time PCR analysis
Antiviral activity against HBV infected in human HepG2.2.15 cells assessed as reduction in cytoplasmic HBV-DNA replication incubated for 8 days by real-time PCR analysis
[PMID: 32692159]
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].

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

HBV-IN-4 Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0838 mL 10.4191 mL 20.8381 mL 52.0953 mL
5 mM 0.4168 mL 2.0838 mL 4.1676 mL 10.4191 mL
10 mM 0.2084 mL 1.0419 mL 2.0838 mL 5.2095 mL
15 mM 0.1389 mL 0.6946 mL 1.3892 mL 3.4730 mL
20 mM 0.1042 mL 0.5210 mL 1.0419 mL 2.6048 mL
25 mM 0.0834 mL 0.4168 mL 0.8335 mL 2.0838 mL
30 mM 0.0695 mL 0.3473 mL 0.6946 mL 1.7365 mL
40 mM 0.0521 mL 0.2605 mL 0.5210 mL 1.3024 mL
50 mM 0.0417 mL 0.2084 mL 0.4168 mL 1.0419 mL
60 mM 0.0347 mL 0.1737 mL 0.3473 mL 0.8683 mL
80 mM 0.0260 mL 0.1302 mL 0.2605 mL 0.6512 mL
100 mM 0.0208 mL 0.1042 mL 0.2084 mL 0.5210 mL
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HBV-IN-4 Related Classifications

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:

HBV-IN-42305897-84-9HBVDNA/RNA SynthesisHepatitis B virusAnti-HBVpharmacokineticoralbioavailabilitylivercapsidadenoassociatedvirusrcDNAssDNAphthalazinoneInhibitorinhibitorinhibit

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