Cat. No.: HY-126970

HBF-0259

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Based on 1 Customer Validation

HBF-0259 is a potent and selective inhibitor of hepatitis B virus (HBV) surface antigen (HBsAg) secretion, with an EC₅₀ of 1.5 μM in HepG2.2.15 cells. HBF-0259 has no effect on HBV DNA synthesis.

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

Purity: 99.99%
CAS No.: 957011-15-3
Formula: C₁₆H₁₂Cl₂FN₅
Molecular Weight:364.20

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

HBF-0259 Chemical Structure

CAS No.: 957011-15-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	EC₅₀	14.2 μM Compound: 5	Antiviral activity against lamivudine/telbivudine-resistant Hepatitis B virus harboring polymerase L528M and M552V mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA Antiviral activity against lamivudine/telbivudine-resistant Hepatitis B virus harboring polymerase L528M and M552V mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA	[PMID: 21786803]
HepG2	EC₅₀	32 μM Compound: 5	Antiviral activity against wild-type Hepatitis B virus infected in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA Antiviral activity against wild-type Hepatitis B virus infected in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA	[PMID: 21786803]
HepG2	EC₅₀	5.5 μM Compound: 5	Antiviral activity against lamivudine/telbivudine-resistant Hepatitis B virus harboring polymerase M552I mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA Antiviral activity against lamivudine/telbivudine-resistant Hepatitis B virus harboring polymerase M552I mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA	[PMID: 21786803]
HepG2	EC₅₀	5.6 μM Compound: 5	Antiviral activity against adefovir-resistant Hepatitis B virus harboring polymerase N584T mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA Antiviral activity against adefovir-resistant Hepatitis B virus harboring polymerase N584T mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA	[PMID: 21786803]
HepG2	EC₅₀	6.4 μM Compound: 5	Antiviral activity against entecavir-resistant Hepatitis B virus harboring polymerase L528M, M552V, T532G and S550I mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA Antiviral activity against entecavir-resistant Hepatitis B virus harboring polymerase L528M, M552V, T532G and S550I mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA	[PMID: 21786803]
HepG2	EC₅₀	9 μM Compound: 5	Antiviral activity against adefovir-resistant Hepatitis B virus harboring polymerase A529V mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA Antiviral activity against adefovir-resistant Hepatitis B virus harboring polymerase A529V mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA	[PMID: 21786803]
HepG2 2.2.15	CC₅₀	>50 μM Compound: 194	Cytotoxicity against human HepG2.2.15 cells by MTT assay Cytotoxicity against human HepG2.2.15 cells by MTT assay	[PMID: 24549242]
HepG2 2.2.15	CC₅₀	>50 μM Compound: 5	Cytotoxicity against human HepG2(2.2.15) cells by MTT assay Cytotoxicity against human HepG2(2.2.15) cells by MTT assay	[PMID: 21786803]
HepG2 2.2.15	EC₅₀	11.3 μM Compound: 5	Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of HBsAg secretion after 6 days by ELISA Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of HBsAg secretion after 6 days by ELISA	[PMID: 21786803]
HepG2 2.2.15	EC₅₀	3 μM Compound: HBF-0259	Antiviral activity against Hepatitis B virus in human HepG2(2.2.15) cells assessed as reduction of large HBsAg secretion after 6 days by densitometric analysis Antiviral activity against Hepatitis B virus in human HepG2(2.2.15) cells assessed as reduction of large HBsAg secretion after 6 days by densitometric analysis	[PMID: 17875990]
HepG2 2.2.15	EC₅₀	4 μM Compound: HBF-0259	Antiviral activity against Hepatitis B virus in human HepG2(2.2.15) cells assessed as reduction of medium HBsAg secretion after 6 days by densitometric analysis Antiviral activity against Hepatitis B virus in human HepG2(2.2.15) cells assessed as reduction of medium HBsAg secretion after 6 days by densitometric analysis	[PMID: 17875990]

In Vitro

HBF-0259 (0.0158-50.0 μM) inhibits the HBsAg secretion (EC₅₀=1.5 μM) in HepDE19 cells, with an CC₅₀ of >50 μM^[1].
HBF-0259 (2-8 μM) significantly reduces the abundance of both L and M in the supernatants of HepG2.2.15 cells^[1].

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

Chemical Information

CAS No. 957011-15-3
Appearance Solid
Molecular Weight 364.20
Formula C₁₆H₁₂Cl₂FN₅
Color White to off-white
SMILES

ClC1=CC=C(C2N=C3N(NN=N3)C(C4=C(F)C=CC=C4Cl)C2)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 (274.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7457 mL

13.7287 mL

27.4574 mL

5 mM

0.5491 mL

2.7457 mL

5.4915 mL

10 mM

0.2746 mL

1.3729 mL

2.7457 mL

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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Dougherty AM, et, al. A substituted tetrahydro-tetrazolo-pyrimidine is a specific and novel inhibitor of hepatitis B virus surface antigen secretion. Antimicrob Agents Chemother. 2007 Dec;51(12):4427-37. [Content Brief]

[2]. Yu W, et, al. Design, synthesis, and biological evaluation of triazolo-pyrimidine derivatives as novel inhibitors of hepatitis B virus surface antigen (HBsAg) secretion. J Med Chem. 2011 Aug 25;54(16):5660-70. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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	2.7457 mL	13.7287 mL	27.4574 mL	68.6436 mL
	5 mM	0.5491 mL	2.7457 mL	5.4915 mL	13.7287 mL
	10 mM	0.2746 mL	1.3729 mL	2.7457 mL	6.8644 mL
	15 mM	0.1830 mL	0.9152 mL	1.8305 mL	4.5762 mL
	20 mM	0.1373 mL	0.6864 mL	1.3729 mL	3.4322 mL
	25 mM	0.1098 mL	0.5491 mL	1.0983 mL	2.7457 mL
	30 mM	0.0915 mL	0.4576 mL	0.9152 mL	2.2881 mL
	40 mM	0.0686 mL	0.3432 mL	0.6864 mL	1.7161 mL
	50 mM	0.0549 mL	0.2746 mL	0.5491 mL	1.3729 mL
	60 mM	0.0458 mL	0.2288 mL	0.4576 mL	1.1441 mL
	80 mM	0.0343 mL	0.1716 mL	0.3432 mL	0.8580 mL
	100 mM	0.0275 mL	0.1373 mL	0.2746 mL	0.6864 mL

Keywords

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HBF-0259

Human Metabolite Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Anti-Infection Compound Library

Antiviral Compound Library

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

HBF-0259

Human Metabolite Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Anti-Infection Compound Library

Antiviral Compound Library

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

HBF-0259 Related Classifications

HY-126970 Related Classifications