1. Membrane Transporter/Ion Channel Anti-infection Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. P2X Receptor Influenza Virus Topoisomerase MicroRNA Apoptosis
  3. Aurintricarboxylic acid

Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM.

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Aurintricarboxylic acid Chemical Structure

Aurintricarboxylic acid Chemical Structure

CAS No. : 4431-00-9

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Based on 1 publication(s) in Google Scholar

Other Forms of Aurintricarboxylic acid:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Aurintricarboxylic acid

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively[1]. Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase[2]. Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis[3]. Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway[4]. Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM[5]. Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM[6].

IC50 & Target[1][3][6]

Topoisomerase II

 

p2x1 Receptor

8.6 nM (IC50)

P2X3 Receptor

72.9 nM (IC50)

Apoptosis

 

miRNA

0.47 μM (IC50)

In Vitro

Aurintricarboxylic acid weakly inhibits P2X2/3Rs, P2X2Rs, P2X4Rs or P2X7Rs[1].
? Aurintricarboxylic acid inhibits ATP-induced currents in a concentration dependent manner[1].
? Aurintricarboxylic acid can inhibit the severe acute respiratory syndrome-associated coronavirus (SARS-CoV) and vaccinia virus[2].
? Aurintricarboxylic acid inhibits replication of influenza A and B viruses by inhibition of neuraminidase activities[2].
? Aurintricarboxylic acid inhibits TWEAK-Fn14-mediated NF-κB activation[4].
? Aurintricarboxylic acid (10 μM; 0.5-2 hours) suppresses TWEAK-Fn14-mediated NF-κB, Akt, and Src phosphorylation in GBM cells[4].
? Aurintricarboxylic acid represses TWEAK-stimulated glioma cell migration and invasion without causing cell cytotoxicity[4].
? Aurintricarboxylic acid (Compound 8) cannot regulate loading of endogenous let-7 onto AGO2 inside cultured cells, whereas can inhibit RISC loading of exogenous siRNA[6].

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

Western Blot Analysis[4]

Cell Line: T98G, A172, GBM44 glioma cells
Concentration: 10 μM
Incubation Time: 0.5 hour, 1 hour, 2 hours
Result: Abrogated TWEAK activation of downstream signals including phosphorylation of the NF-κB family member p65, Akt, and Src in all three GBM cell lines.
Molecular Weight

422.34

Formula

C22H14O9

CAS No.
Appearance

Solid

Color

Brown to black

SMILES

O=C(C=C/1)C(C(O)=O)=CC1=C(C2=CC(C(O)=O)=C(O)C=C2)\C3=CC(C(O)=O)=C(O)C=C3

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 : 125 mg/mL (295.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

NH4OH : 10 mg/mL (23.68 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3678 mL 11.8388 mL 23.6776 mL
5 mM 0.4736 mL 2.3678 mL 4.7355 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

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Volume (start)

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C2

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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: ≥ 2.08 mg/mL (4.92 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.

    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: ≥ 2.08 mg/mL (4.92 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 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

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(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

Purity: ≥92.0%

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
NH4OH / DMSO 1 mM 2.3678 mL 11.8388 mL 23.6776 mL 59.1940 mL
5 mM 0.4736 mL 2.3678 mL 4.7355 mL 11.8388 mL
10 mM 0.2368 mL 1.1839 mL 2.3678 mL 5.9194 mL
15 mM 0.1579 mL 0.7893 mL 1.5785 mL 3.9463 mL
20 mM 0.1184 mL 0.5919 mL 1.1839 mL 2.9597 mL
DMSO 25 mM 0.0947 mL 0.4736 mL 0.9471 mL 2.3678 mL
30 mM 0.0789 mL 0.3946 mL 0.7893 mL 1.9731 mL
40 mM 0.0592 mL 0.2960 mL 0.5919 mL 1.4799 mL
50 mM 0.0474 mL 0.2368 mL 0.4736 mL 1.1839 mL
60 mM 0.0395 mL 0.1973 mL 0.3946 mL 0.9866 mL
80 mM 0.0296 mL 0.1480 mL 0.2960 mL 0.7399 mL
100 mM 0.0237 mL 0.1184 mL 0.2368 mL 0.5919 mL
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  • 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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Aurintricarboxylic acid
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