1. Apoptosis Metabolic Enzyme/Protease Anti-infection
  2. Apoptosis Endogenous Metabolite Antibiotic
  3. Citric acid

Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice.

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Citric acid Chemical Structure

Citric acid Chemical Structure

CAS No. : 77-92-9

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Description

Citric acid is a natural preservative and food tartness enhancer. Citric acid induces apoptosis and cell cycle arrest at G2/M phase and S phase in HaCaT cells. Citric acid cause oxidative damage of the liver by means of the decrease of antioxidative enzyme activities. Citric acid causes renal toxicity in mice[1][2][3].

IC50 & Target

Human Endogenous Metabolite

 

In Vitro

Citric acid (0-12.5 mM; 24 h) shows antiproliferative activity in a dose dependent manner[3].
Citric acid (12.5 mM; 72 h) induces apoptosis and cell cycle arrest at G2/M phase and S phase in a dosedependent manner[3].
Citric acid (12.5 mM; 48 h) increases the expression of FAS, BAX, BID, AIF, EndoG, cytochrome c, PARP, GADD153, GRP78 and caspase-3, -8, -9, and decreases of BCL-2 and BCL-Xl[3].

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

Cell Viability Assay[3]

Cell Line: HaCaT cells
Concentration: 0, 2.5, 5, 7.5, 10, 12.5 mM
Incubation Time: 24 h
Result: Inhibited the cell viability in a dose dependent manner.

Cell Cytotoxicity Assay[3]

Cell Line: HaCaT cells
Concentration: 12.5 mM
Incubation Time: 0, 12, 24, 48, 72 h
Result: Induced apoptosis and cell cycle arrest at G2/M phase and S phase in a dosedependent manner.

Western Blot Analysis[3]

Cell Line: HaCaT cells
Concentration: 12.5 mM
Incubation Time: 12, 24, 48 h
Result: Increased the expression of FAS, BAX, BID, AIF, EndoG, cytochrome c, PARP, GADD153, GRP78 and caspase-3, -8, -9, and decreased of BCL-2 and BCL-Xl.
In Vivo

Citric acid (120, 240, and 480 mg/kg; i.p.) significantly decreases GSH-Px activity and induces an increase in the MDA (malonyldialdehyde) levels in mouse liver[1].
Citric acid (120, 240, and 480 mg/kg; i.p.) induces apoptosis by increases caspase-3 activity in a dose-dependent manner in mouse hepatocytes[1].
Citric acid (120, 240, and 480 mg/kg; i.p.; weekly for 3 weeks) causes renal toxicity in mice[2].

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

Animal Model: 20 g male Kunming mice[2]
Dosage: 120, 240, 480 mg/kg
Administration: I.p.; weekly for 3 weeks
Result: T-SOD and GSH-Px activities in the treated groups decreased with increasing doses of citric acid, NOS activity tended to increase, and H2O2 and MDA contents gradually decreased.
Clinical Trial
Molecular Weight

192.12

Formula

C6H8O7

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

OC(CC(CC(O)=O)(C(O)=O)O)=O

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (520.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (520.51 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.2051 mL 26.0254 mL 52.0508 mL
5 mM 1.0410 mL 5.2051 mL 10.4102 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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 (13.01 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 (13.01 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 100 mg/mL (520.51 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: ≥98.0%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 5.2051 mL 26.0254 mL 52.0508 mL 130.1270 mL
5 mM 1.0410 mL 5.2051 mL 10.4102 mL 26.0254 mL
10 mM 0.5205 mL 2.6025 mL 5.2051 mL 13.0127 mL
15 mM 0.3470 mL 1.7350 mL 3.4701 mL 8.6751 mL
20 mM 0.2603 mL 1.3013 mL 2.6025 mL 6.5064 mL
25 mM 0.2082 mL 1.0410 mL 2.0820 mL 5.2051 mL
30 mM 0.1735 mL 0.8675 mL 1.7350 mL 4.3376 mL
40 mM 0.1301 mL 0.6506 mL 1.3013 mL 3.2532 mL
50 mM 0.1041 mL 0.5205 mL 1.0410 mL 2.6025 mL
60 mM 0.0868 mL 0.4338 mL 0.8675 mL 2.1688 mL
80 mM 0.0651 mL 0.3253 mL 0.6506 mL 1.6266 mL
100 mM 0.0521 mL 0.2603 mL 0.5205 mL 1.3013 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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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Citric acid
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