Art. -Nr.: HY-76938

Actarit

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

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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.

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Reinheit: 99.58%
CAS. Nr.: 18699-02-0
Formel: C₁₀H₁₁NO₃
Molecular Weight:193.20

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Actarit Chemical Structure

CAS. Nr.: 18699-02-0

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Biologische Aktivität
- Beschreibung
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle Carbonic Anhydrase Isoform-spezifische Produkte anzeigen :

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

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.

Chemical Information

CAS. Nr. 18699-02-0
Appearance Solid
Molecular Weight 193.20
Formel C₁₀H₁₁NO₃
Color Off-white to brown
SMILES

O=C(C)NC(C=C1)=CC=C1CC(O)=O
Synonyms

4-Acetylaminophenylacetic acid; MS-932
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

5.1760 mL

25.8799 mL

51.7598 mL

5 mM

1.0352 mL

5.1760 mL

10.3520 mL

10 mM

0.5176 mL

2.5880 mL

5.1760 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kawai K, et al. Suppressive effects of 4-acetylaminophenylacetic acid (actarit) on experimental autoimmune encephalomyelitis in rats. Immunopharmacology. 1998 May;39(2):127-38. [Content Brief]

[2]. Fujisawa H, et al. Effect of actarit on type II collagen-induced arthritis in mice. Arzneimittel-forschung, 01 Jan 1994, 44(1):64-68. [Content Brief]

[3]. Ghislat G, et al. Identification and Validation of Carbonic Anhydrase II as the First Target of the Anti-Inflammatory Drug Actarit. Biomolecules. 2020 Nov 19;10(11):1570. [Content Brief]

[4]. Fujisawa H, et al. Suppressive effect of actarit on IgA production in mice: activation of CD4+ suppressor T-cells in Peyer's patches. Int J Immunopharmacol. 1995 Jul;17(7):611-7. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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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Actarit

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Alle Carbonic Anhydrase Isoform-spezifische Produkte anzeigen

Alle TNF Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Actarit Related Classifications

HY-76938 Related Classifications