1. AT-130

AT-130, a phenylpropenamide derivative, is a potent hepatitis B virus (HBV) replication non-nucleoside inhibitor. AT-130 inhibits the viral DNA synthesis with an EC50 of 0.13 μM. AT-130 inhibits both wt and mutant HBVs. AT-130 has anti-HBV activity in hepatoma cells.

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AT-130 Chemical Structure

AT-130 Chemical Structure

CAS No. : 211364-06-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE AT-130

  • Biological Activity

  • Purity & Documentation

  • Customer Review

Description

AT-130, a phenylpropenamide derivative, is a potent hepatitis B virus (HBV) replication non-nucleoside inhibitor. AT-130 inhibits the viral DNA synthesis with an EC50 of 0.13 μM. AT-130 inhibits both wt and mutant HBVs. AT-130 has anti-HBV activity in hepatoma cells[1][2][3].

In Vitro

AT-130 inhibits Wt HBV (IC50=2.4 μM), rtL180M HBV (IC50=9.8 μM), rtM204I HBV (IC50=35.6 μM)[1].
AT-130 (0.1, 1, 5, 10, 100 μM; for 7 days) causes dose-dependent inhibition of wt HBV replication in HepG2 cells transduced with HBV baculovirus. AT-130 at a concentration of 2.5 μM, reduces encapsidated HBV DNA by 50% (IC50) and at 18.5 μM by 90% (IC90)[1].
AT-130 has no toxic to either HepG2 or Huh-7 cells at concentrations of up to 250 μM[1].
AT-130 (0.005, 0.05, 0.5, 5, 50 μM) does not inhibit HBV DNA synthesis by blocking the HBV endogenous DNA polymerase reaction directly in Huh 7 or HepG2 cells. AT-130 inhibits HBV DNA replication in hepatoma cells but has no effect on viral DNA polymerase activity or core protein translation[3].
AT-130 (2.5, 18.5 μM) has no effect on total HBV RNA production but does reduce encapsidated RNA. AT-130 does not affect core protein or nucleocapsid production and the activity of the protein expression vector[3].

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

Clinical Trial
Molecular Weight

488.33

Formula

C22H22BrN3O5

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N/C(C(N1CCCCC1)=O)=C(Br)\C2=CC=CC=C2OC)C3=CC=C([N+]([O-])=O)C=C3

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 : 25 mg/mL (51.19 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 2.0478 mL 10.2390 mL 20.4780 mL
5 mM 0.4096 mL 2.0478 mL 4.0956 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
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Concentration
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Volume
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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

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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 2.0478 mL 10.2390 mL 20.4780 mL 51.1949 mL
5 mM 0.4096 mL 2.0478 mL 4.0956 mL 10.2390 mL
10 mM 0.2048 mL 1.0239 mL 2.0478 mL 5.1195 mL
15 mM 0.1365 mL 0.6826 mL 1.3652 mL 3.4130 mL
20 mM 0.1024 mL 0.5119 mL 1.0239 mL 2.5597 mL
25 mM 0.0819 mL 0.4096 mL 0.8191 mL 2.0478 mL
30 mM 0.0683 mL 0.3413 mL 0.6826 mL 1.7065 mL
40 mM 0.0512 mL 0.2560 mL 0.5119 mL 1.2799 mL
50 mM 0.0410 mL 0.2048 mL 0.4096 mL 1.0239 mL
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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.

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AT-130
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HY-100028
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