2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Cytoskeleton NF-κB
  3. PPAR PAK NF-κB Endogenous Metabolite
  4. 5-Aminosalicylic Acid

5-Aminosalicylic Acid  (Synonyms: Mesalamine; 5-ASA; Mesalazine)

Cat. No.: HY-15027 Purity: 99.82%
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5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

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

5-Aminosalicylic Acid Chemical Structure

5-Aminosalicylic Acid Chemical Structure

CAS No. : 89-57-6

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500 mg USD 55 In-stock
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Based on 16 publication(s) in Google Scholar

Other Forms of 5-Aminosalicylic Acid:

5-Aminosalicylic Acid Related Antibodies

Top Publications Citing Use of Products

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PPARα PPARβ/δ PPARγ PPAR PPARδ

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PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB. 5-Aminosalicylic acid can inhibit the activity of osteopontin (OPN).

IC50 & Target[1]

PPARγ

 

PAK1

 

p65

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
> 15 mM
Compound: 12
Cytotoxicity against HEK293 cells harboring pendrin P123S mutant after 72 hrs by MTT assay
Cytotoxicity against HEK293 cells harboring pendrin P123S mutant after 72 hrs by MTT assay
[PMID: 28341401]
HT-29 IC50
18.1 mM
Compound: 5-ASA
Antiinflammatory activity in human HT-29 cells assessed as inhibition of TNF-alpha induced BCECF-AM labeled human U937 cell adhesion preincubated for 1 hr followed by stimulation with TNF-alpha for 3 hrs followed by further co-incubation with BCECF-AM lab
Antiinflammatory activity in human HT-29 cells assessed as inhibition of TNF-alpha induced BCECF-AM labeled human U937 cell adhesion preincubated for 1 hr followed by stimulation with TNF-alpha for 3 hrs followed by further co-incubation with BCECF-AM lab
[PMID: 27597248]
HT-29 IC50
20.4 mM
Compound: 5-ASA
Inhibition of TNF-alpha-induced adhesion of BCECF-labeled human U937 cells to human HT-29 cells preincubated for 1 hr followed by TNF-alpha challenge measured after 3 hrs by fluorescence microscopic method
Inhibition of TNF-alpha-induced adhesion of BCECF-labeled human U937 cells to human HT-29 cells preincubated for 1 hr followed by TNF-alpha challenge measured after 3 hrs by fluorescence microscopic method
[PMID: 28646757]
U-87MG ATCC IC50
> 1000 μM
Compound: 4
Inhibition of xc-cystine-glutamate antiporter-mediated cystine uptake in human U87 cells using L-[14C]cystine as substrate after 15 mins by liquid scintillation counting
Inhibition of xc-cystine-glutamate antiporter-mediated cystine uptake in human U87 cells using L-[14C]cystine as substrate after 15 mins by liquid scintillation counting
[PMID: 21889337]
In Vitro

5-Aminosalicylic acid (5-ASA) is a specific agonist for PPARγ, and only PPARγ but not PPARα or PPARδ induces p65 degradation. 5-Aminosalicylic acid induces degradation of p65 protein indicative of PPARγ's E3 ubiquitin ligase activity. 5-Aminosalicylic acid also inhibits PAK1 at the mRNA level which is suggestive of an additional mechanism independent of PPARγ ligand activation. 5-Aminosalicylic acid blocks NF-κB in intestinal epithelial cells (IECs) through inhibition of PAK1[1]. Pretreatment with 5-Aminosalicylic acid (5-ASA) or Nimesulide at different concentration (10-1000 μmol/L) for 12-96 h, inhibits the growth of HT-29 colon carcinoma cells in a dose and time-dependent manner. However, the suppression of 5-Aminosalicylic acid or Nimesulide has no statistical significance. The growth of HT-29 colon carcinoma cells is inhibited dose-dependently when pretreated with different doses of combined 5-Aminosalicylic acid and Nimesulide. Combined 5-Aminosalicylic acid (final concentration 100 μM) and Nimesulide (final concentration 10-1000 μM) inhibits the proliferation of HT-29 colon carcinoma cells in a dose-dependent manner, being more potent than corresponding dose of Nimesulide. Similarly, combined Nimesulide (final concentration 100 μM) and 5-Aminosalicylic acid (final concentration 10-1000 μM) also inhibits the proliferation of these cells dose-dependently, being more potent than corresponding dose of 5-Aminosalicylic acid[2].

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

5-Aminosalicylic Acid Related Antibodies
In Vivo

5-Aminosalicylic acid (5-ASA) has an antineoplastic effect in a xenograft tumor model. To evaluate the in vivo antineoplasic effect of 5-Aminosalicylic acid, SCID mice engrafted with HT-29 colon cancer cells are treated daily for 21 consecutive days with 5-Aminosalicylic acid at 50 mM. At the end of the treatment, a reduction of 80-86% of tumor weight and volume is observed in SCID mice receiving 5-Aminosalicylic acid compared with control mice or mice treated with GW9662 alone. The antineoplastic effect of 5-Aminosalicylic acid is already detectable after 10 days of 5-Aminosalicylic acid treatment. Similar results are obtained with mice treated with 5-Aminosalicylic acid at 5 mM. Antitumorigenic effect of 5-Aminosalicylic acid is completely abolished at 21 days by simultaneous intraperitoneal administration of GW9662. Thus, the observed antineoplastic effect of 5-Aminosalicylic acid is at least partially dependent on PPARγ[3].

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

153.14

Formula

C7H7NO3
CAS No.
Appearance

Solid

Color

Brown to gray

SMILES

OC1=C(C(O)=O)C=C(N)C=C1
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

RT, protect from light, stored under nitrogen

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

DMSO : 66.67 mg/mL (435.36 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)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 6.5301 mL 32.6505 mL 65.3010 mL
5 mM 1.3060 mL 6.5301 mL 13.0602 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.

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

Mass
=
Concentration
×
Volume
×
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

×
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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (16.33 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 (16.33 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:  50% PEG300    50% Saline

    Solubility: 7.14 mg/mL (46.62 mM); Suspended solution; Need ultrasonic

  • Protocol 2

    Add each solvent one by one:  0.5% CMC-Na/saline water

    Solubility: 16.67 mg/mL (108.86 mM); Suspended solution; Need ultrasonic

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

Purity: 99.82%

SDS (393 KB)

COA (252 KB) HNMR (244 KB) RP-HPLC (276 KB) MS (68 KB)

Handling Instructions (2659 KB)
References
Cell Assay
[2]

Cytostatic effects are measured by MTT assay. HT-29 colon carcinoma cells are detached with a 0.25% trypsin solution for 5 min. Subsequently, the cells are seeded onto 96-well plates (1×106 cells/well), supplemented with 10% FCS and allowed to attach for 24 h before the addition of test compounds (5-Aminosalicylic acid 10, 50, 100, 500, and 1000 μM; Nimesulide; and their combination). Test compounds are diluted in serum-free culture medium. Then the cells are incubated in a medium or at different concentrations of drugs for 48 h, 20 μL of MTT solution (5 g/L) in PBS is added. Four hours later, the medium in each well is removed, and 120 μL of 0.04 mM muriatic isopropanol is added, slightly concussed for 10 min. Dye uptake is measured at 490 nm with an ELISA reader. Five wells are used for each concentration or as a control group. On the other hand, the cells are seeded onto 96-well plates (1×106 cells/well) and allowed to attach for 24 h, then treated with test compounds (5-Aminosalicylic acid, Nimesulide, and their combination). The final concentration is 100 μM. The same medium is added into the control group and dye uptake is then measured. Five wells are used for each test compound or control group[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Mice[3]
Six to seven weeks old pathogen-free BALB/c SCID mice are used. Human colon cancer cells (107 HT-29 cells) pretreated or not with GW9662 for 24 h are implanted subcutaneously in the flank of animals. Two days after cell inoculation, mice are treated with 5-Aminosalicylic acid (5 or 50 mM) administered daily by peritumoral injection for 10 or 21 days. The effect of PPARγ during 5-Aminosalicylic acid treatment is evaluated by daily intraperitoneal injection of GW9662 (1 mg/kg/day). The control group receives saline instead of 5-Aminosalicylic acid. Mice are checked three times a week for tumor development. After killing at 10 or 21 days, tumor size and volume are calculated. Tumors are weighted before paraffin embedding for histological examination.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 1 mM 6.5301 mL 32.6505 mL 65.3010 mL 163.2525 mL
5 mM 1.3060 mL 6.5301 mL 13.0602 mL 32.6505 mL
10 mM 0.6530 mL 3.2651 mL 6.5301 mL 16.3253 mL
15 mM 0.4353 mL 2.1767 mL 4.3534 mL 10.8835 mL
20 mM 0.3265 mL 1.6325 mL 3.2651 mL 8.1626 mL
25 mM 0.2612 mL 1.3060 mL 2.6120 mL 6.5301 mL
30 mM 0.2177 mL 1.0884 mL 2.1767 mL 5.4418 mL
40 mM 0.1633 mL 0.8163 mL 1.6325 mL 4.0813 mL
50 mM 0.1306 mL 0.6530 mL 1.3060 mL 3.2651 mL
60 mM 0.1088 mL 0.5442 mL 1.0884 mL 2.7209 mL
80 mM 0.0816 mL 0.4081 mL 0.8163 mL 2.0407 mL
100 mM 0.0653 mL 0.3265 mL 0.6530 mL 1.6325 mL
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5-Aminosalicylic Acid 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.

Keywords:

5-Aminosalicylic Acid89-57-6Mesalamine 5-ASA MesalazinePPARPAKNF-κBEndogenous MetabolitePeroxisome proliferator-activated receptorsp21 activated kinasesNuclear factor-κBNuclear factor-kappaBInhibitorinhibitorinhibit

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