2. Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  3. Carbonic Anhydrase TNF Receptor IFNAR
  4. Actarit

Actarit  (Synonyms: 4-Acetylaminophenylacetic acid; MS-932)

Cat. No.: HY-76938 Purity: 99.58%
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Actarit (4-Acetylaminophenylacetic acid) is an orally active Carbonic Anhydrase II (CAII) inhibitor with an IC50 of 422 nM. Actarit shows suppressive effects experimental autoimmune encephalomyelitis in rats. Actarit inhibits the development of type ll collagen (CII)-induced arthritis in mice by suppressing delayed-type hypersensitivity to CII. Actarit can be used for the study of Multiple Sclerosis (MS) and rheumatoid arthritis.

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

Actarit

Actarit Chemical Structure

CAS No. : 18699-02-0

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Based on 1 publication(s) in Google Scholar

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Actarit Related Antibodies

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  • Purity & Documentation

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  • Customer Review

Description

Actarit (4-Acetylaminophenylacetic acid) is an orally active Carbonic Anhydrase II (CAII) inhibitor with an IC50 of 422 nM. Actarit shows suppressive effects experimental autoimmune encephalomyelitis in rats. Actarit inhibits the development of type ll collagen (CII)-induced arthritis in mice by suppressing delayed-type hypersensitivity to CII. Actarit can be used for the study of Multiple Sclerosis (MS) and rheumatoid arthritis[1][2][3][4].

In Vivo

Actarit (300 mg/kg, i.p., from day 8 to 14 after immunization or day 0 to 7 after cell transfer) shows suppressive effects on clinical manifestations and pathological findings of both actively induced and adoptively transferred experimental autoimmune encephalomyelitis in Lewis rats[1].
Actarit (3-300 mg/kg, p.o., once daily, 4 days) activates CD4+ suppressor T-cells in the Peyer's patches (PP), resulting in a specific suppression of IgA production after LPS (HY-D1056) stimulation in mice[4].

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

Animal Model: Naive male Lewis rats (2-3 months old) were subcutaneously inoculated with 75 mg of guinea-pig myelin basic protein peptide 68-86 in complete Freund’s adjuvant containing 5 mg/ml of H37RA into the hind footpads to induce actively induced experimental autoimmune encephalomyelitis[1]
Dosage: 30, 100, 300, 600 mg/kg
Administration: i.p., from day 8 to 14 after immunization
Result: Suppressed clinical symptoms.
Reduced the number of infiltrating cells in the central nervous system (CNS).
Decreased the percentages of CD4+ and CD25+ positive cells in the CNS.
Reduced the total number of infiltrating cells in the spinal cord and the number of splenocytes on day 14.
Downregulated the mRNA expression of TNF-α and IFN-γ in the spinal cord on day 14 and 17.
Upregulated the mRNA expression of IL-10 in the spleen on day 17.
Doses of 30 and 100 mg/kg had no significant effect on the clinical course; 600 mg/kg could delay the onset and reduce severity, but without statistical significance.
Administration from day 0 to 7 after immunization or from 3 days before immunization to day 5 after immunization had no significant effect on the clinical course.
Animal Model: Male Lewis rats (3-4 months old) were immunized with 75 mg of myelin basic protein peptide in complete Freund’s adjuvant; 9-10 days later, regional lymph node cells were isolated, cultured with 7.5 mg/mL of the peptide, activated lymphoblasts were separated, and each rat was intraperitoneally injected with 15 × 106 lymphoblasts to establish adoptively transferred experimental autoimmune encephalomyelitis model[1]
Dosage: 300 mg/kg
Administration: i.p. at day 0 to 7 after cell transfer
Result: Suppressed clinical symptoms.
Animal Model: Male BALB/c mice[4]
Dosage: 3, 30, 300 mg/kg
Administration: p.o. once daily for 4 days
Result: Suppressd IgA production (not IgM and IgG) by LPS-stimulated B cells, with the effect abrogated by CD4⁺ cell depletion.
Did not affect serum IgA levels, gut IgA secretion in LPS-unstimulated mice, or PP lymphocyte subsets (Thy-1+, CD4+/CD8+ percentages).
Had no impact on B-cell proliferative responses to LPS or anti-μ-chain antibody plus rIL-4.
Molecular Weight

193.20

Formula

C10H11NO3
CAS No.
Appearance

Solid

Color

Off-white to brown

SMILES

O=C(C)NC(C=C1)=CC=C1CC(O)=O
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 : 100 mg/mL (517.60 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 5.1760 mL 25.8799 mL 51.7598 mL
5 mM 1.0352 mL 5.1760 mL 10.3520 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.

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  • 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)

V1

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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (12.94 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (12.94 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 +
% 
+
%
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%
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 5.1760 mL 25.8799 mL 51.7598 mL 129.3996 mL
5 mM 1.0352 mL 5.1760 mL 10.3520 mL 25.8799 mL
10 mM 0.5176 mL 2.5880 mL 5.1760 mL 12.9400 mL
15 mM 0.3451 mL 1.7253 mL 3.4507 mL 8.6266 mL
20 mM 0.2588 mL 1.2940 mL 2.5880 mL 6.4700 mL
25 mM 0.2070 mL 1.0352 mL 2.0704 mL 5.1760 mL
30 mM 0.1725 mL 0.8627 mL 1.7253 mL 4.3133 mL
40 mM 0.1294 mL 0.6470 mL 1.2940 mL 3.2350 mL
50 mM 0.1035 mL 0.5176 mL 1.0352 mL 2.5880 mL
60 mM 0.0863 mL 0.4313 mL 0.8627 mL 2.1567 mL
80 mM 0.0647 mL 0.3235 mL 0.6470 mL 1.6175 mL
100 mM 0.0518 mL 0.2588 mL 0.5176 mL 1.2940 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.

Keywords:

Actarit18699-02-04-Acetylaminophenylacetic acid MS-932MS932MS 932MS-932Carbonic AnhydraseTNF ReceptorIFNARCarbonate dehydrataseTumor Necrosis Factor ReceptorTNFRInterferon-α/β receptorInterferon-alpha/beta receptorDMARDInhibitorinhibitorinhibit

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