Actarit
Based on 1 Customer Validation
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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- Pureza: 99.58%
- No. CAS: 18699-02-0
- Fòrmula: C10H11NO3
- Peso molecular:193.20
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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.
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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]
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Dosage:30, 100, 300, 600 mg/kg
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Administration:i.p., from day 8 to 14 after immunization
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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.
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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]
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Dosage:300 mg/kg
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Administration:i.p. at day 0 to 7 after cell transfer
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Result:Suppressed clinical symptoms.
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Animal Model:Male BALB/c mice[4]
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Dosage:3, 30, 300 mg/kg
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Administration:p.o. once daily for 4 days
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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
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No. CAS 18699-02-0
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Appearance Solid
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Peso molecular 193.20
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Fòrmula C10H11NO3
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Color Off-white to brown
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SMILES
O=C(C)NC(C=C1)=CC=C1CC(O)=O
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Synonyms
4-Acetylaminophenylacetic acid; MS-932
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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 |
Actarit Related Classifications
HY-76938 Related Classifications
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