1. Anti-infection
  2. HBV
  3. GST-HG131

GST-HG131 is a specific inbihitor of hepatitis B virus (HBV) surface antigen, belongs to dihydrobenzopyridooxazepine (DBP) series. GST-HG131 exhibits excellent and specific HBV antigens inhibition with EC50 of 28.2 nM (HBsAg) and 16.0 nM (HBeAg), respectively, but also it is safety for animal.

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

GST-HG131 Chemical Structure

GST-HG131 Chemical Structure

CAS No. : 2270215-69-3

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5 mg USD 480 In-stock
10 mg USD 800 In-stock
25 mg USD 1650 In-stock
50 mg USD 2600 In-stock
100 mg USD 4000 In-stock
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500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

GST-HG131 is a specific inbihitor of hepatitis B virus (HBV) surface antigen, belongs to dihydrobenzopyridooxazepine (DBP) series. GST-HG131 exhibits excellent and specific HBV antigens inhibition with EC50 of 28.2 nM (HBsAg) and 16.0 nM (HBeAg), respectively, but also it is safety for animal[1].

IC50 & Target

EC50: 28.2 nM (HBsAg); 16.0 nM (HBeAg)[1]

In Vitro

GST-HG131 shows moderate permeability in Caco-2 assay, low rat and human plasma protein binding, low clearance in liver microsomal stability assays[1].
GST-HG131 shows antiviral activity in primary human hepatocytes (PHH) expressing HBV, inhibits HBV antigens (both HBsAg and HBeAg)[1].
GST-HG131 (500 nM) appears to inhibit HBV antigens through inhibition of HBV RNAs in a dose- and time-dependent manner[1].
GST-HG131 shows specific HBV inhibition over other viruses, such as hepatitis C virus, herpes simplex virus type 1 and influenza virus H1N1[1].

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

Western Blot Analysis[1]

Cell Line: Northern-Blot
Concentration: 500, 166.67, 55.56, 18.52, 6.17, 2.06, 0.68, 0.23, and 0 nM
Incubation Time: 4, 8, 16, 24, 48 hours
Result: Inhibited HBV antigens through inhibition of HBV RNAs.
In Vivo

GST-HG131 exhibits low clearance, moderate plasma half-life (T1/2), high plasma exposure (Cmax and AUC) and oral bioavailability[1].
GST-HG131 (3, 10, and 30 mg/kg; i.v., tail vein injection; once daily for 4 weeks) shows HBV inhibition in an AAV/HBV mouse model[1].
GST-HG131 (100, 300, and 1000 mg/kg; p.o.; once daily for 14 d) is well tolerated at 300 mg/kg and 100 mg/kg in rat preliminary toxicology study[1].
PK parameter in mouse, rat, and dog[1]
Note: Male C57BL/6 mice (iv/po: 0.5 mg/kg), male SD rats (iv/po: 0.5 mg/kg) and Beagle dogs (iv/po: 0.33 mg/kg).

Parameter CL(iv) (mL/min/kg) Vdss(iv) (L/kg) T1/2 (h) Cmax(po) (nM) AUC0-last(po) (nM·h) Bioavailability (F%)
Mouse 75 5.8 2.5 1055 876 91.6
Rat 28 1.72 2.0 659 1832 71.1
Dog 4.04 1.08 3.39 4850 26500 93.2

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

Molecular Weight

431.48

Formula

C23H29NO7

CAS No.
Appearance

Solid

Color

Light yellow to light brown

SMILES

O=C(C1=CN2[C@H](C(C)(C)C)COC3=CC(OCCCOC)=C(OC)C=C3C2=CC1=O)O

Shipping

Room temperature in continental US; may vary elsewhere.

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

DMSO : 100 mg/mL (231.76 mM; ultrasonic and warming and heat to 60°C; 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 2.3176 mL 11.5880 mL 23.1760 mL
5 mM 0.4635 mL 2.3176 mL 4.6352 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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 (5.79 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 (5.79 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 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:

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g

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(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 2.3176 mL 11.5880 mL 23.1760 mL 57.9401 mL
5 mM 0.4635 mL 2.3176 mL 4.6352 mL 11.5880 mL
10 mM 0.2318 mL 1.1588 mL 2.3176 mL 5.7940 mL
15 mM 0.1545 mL 0.7725 mL 1.5451 mL 3.8627 mL
20 mM 0.1159 mL 0.5794 mL 1.1588 mL 2.8970 mL
25 mM 0.0927 mL 0.4635 mL 0.9270 mL 2.3176 mL
30 mM 0.0773 mL 0.3863 mL 0.7725 mL 1.9313 mL
40 mM 0.0579 mL 0.2897 mL 0.5794 mL 1.4485 mL
50 mM 0.0464 mL 0.2318 mL 0.4635 mL 1.1588 mL
60 mM 0.0386 mL 0.1931 mL 0.3863 mL 0.9657 mL
80 mM 0.0290 mL 0.1449 mL 0.2897 mL 0.7243 mL
100 mM 0.0232 mL 0.1159 mL 0.2318 mL 0.5794 mL
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GST-HG131 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.

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GST-HG131
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