| Size | Price | |
|---|---|---|
| Other Sizes |
| Targets |
Synovial cells (TNF-α and IL-1β secretion); malarial parasite plastid. Actarit reduces spontaneous TNF-α and IL-1β secretion by primary synovial cells of patients with rheumatoid arthritis. It inhibits the development of type II collagen-induced arthritis by suppressing delayed-type hypersensitivity to collagen. The compound also inhibits the malarial parasite plastid with a potency of 4256.2 nM.
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|---|---|
| ln Vitro |
Actarit inhibits spontaneous TNF-α and IL-1β secretion by primary synovial cells of patients with rheumatoid arthritis in vitro. It has been shown to suppress disease activity in cell-based assays using synovial cells from rheumatoid arthritis patients. The compound's anti-inflammatory activity has been characterized in various in vitro assays measuring cytokine production and immune cell function.
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| ln Vivo |
In vivo, Actarit inhibits the development of type II collagen-induced arthritis in DBA/1J mice by suppressing delayed-type hypersensitivity to collagen. It can be used for the study of multiple sclerosis and rheumatoid arthritis. The compound is administered orally and has been studied in animal models of autoimmune and inflammatory diseases.
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| Enzyme Assay |
In vitro cytokine assays for Actarit involve culturing primary synovial cells from rheumatoid arthritis patients. Cells are treated with Actarit at varying concentrations (typically 1-100 µM) for 24-48 hours. TNF-α and IL-1β levels in the culture supernatant are measured by ELISA. The compound's ability to reduce spontaneous cytokine secretion is assessed. Cell viability is assessed using standard assays such as MTT.
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| Cell Assay |
In vitro cellular assays for Actarit involve culturing synovial cells or immune cells. Cells are treated with Actarit at varying concentrations, and inflammatory cytokine production (TNF-α, IL-1β, IL-6) is measured by ELISA or multiplex assays. NF-κB activation can be assessed by measuring IκBα phosphorylation or NF-κB DNA binding. The compound's effects on immune cell proliferation and activation can also be assessed.
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| Animal Protocol |
In vivo animal studies for Actarit are conducted in mouse models of type II collagen-induced arthritis. DBA/1J mice are immunized with type II collagen and treated with Actarit orally. Arthritis severity is assessed by clinical scoring, paw swelling measurements, and histological evaluation of joint inflammation and cartilage destruction. Delayed-type hypersensitivity to collagen is assessed by measuring ear swelling responses.
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| ADME/Pharmacokinetics |
Actarit has a molecular weight of 193.20 g/mol and a molecular formula of C10H11NO3. It is soluble in DMSO at 33 mg/mL (170.8 mM). The compound should be stored at -20°C protected from light. It is available with a purity of ≥98%. Detailed pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution are not extensively documented.
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| Toxicity/Toxicokinetics |
Actarit is generally well-tolerated at therapeutic doses but can cause side effects including gastrointestinal disturbances, skin reactions, and liver enzyme elevations. It is contraindicated in patients with severe hepatic or renal impairment. The compound is approved for clinical use in some countries for the treatment of rheumatoid arthritis. Standard safety precautions should be taken when handling the compound.
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| Additional Infomation |
Actarit is an aniline compound, belonging to the acetamide class of compounds.
Actarit (MS-932) is an antirheumatic drug that reduces spontaneous TNF-α and IL-1β secretion by synovial cells and inhibits type II collagen-induced arthritis in mice. It is used for the treatment of rheumatoid arthritis and has been studied for multiple sclerosis. The compound is approved for clinical use in some countries and is available as a prescription medication. |
| Molecular Formula |
C10H11NO3
|
|---|---|
| Molecular Weight |
193.2
|
| Exact Mass |
193.073
|
| CAS # |
18699-02-0
|
| PubChem CID |
2018
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| Appearance |
Off-white to brown solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
449.1±28.0 °C at 760 mmHg
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| Melting Point |
173-175°C
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| Flash Point |
225.4±24.0 °C
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| Vapour Pressure |
0.0±1.2 mmHg at 25°C
|
| Index of Refraction |
1.605
|
| LogP |
0.37
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
14
|
| Complexity |
219
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O([H])C(C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])N([H])C(C([H])([H])[H])=O)=O
|
| InChi Key |
MROJXXOCABQVEF-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C10H11NO3/c1-7(12)11-9-4-2-8(3-5-9)6-10(13)14/h2-5H,6H2,1H3,(H,11,12)(H,13,14)
|
| Chemical Name |
2-(4-acetamidophenyl)acetic acid
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| Synonyms |
Actarit NSC 170317 NSC170317NSC-170317
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~517.60 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (12.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.5176 mL | 2.5880 mL | 5.1760 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03660059 | Completed | Drug: Peficitinib Drug: Plaebo |
Rheumatoid Arthritis (RA) | Astellas Pharma China, Inc. | September 27, 2018 | Phase 3 |
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