Actarit
(Synonyms: 阿克他利,4-Acetylaminophenylacetic acid; MS-932) 目录号 : GC40645
An anti-inflammatory agent
Cas No.:18699-02-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Actarit is an orally active immunomodulator that reduces symptoms in animal models and clinical trials of rheumatoid arthritis. It suppresses inflammation and nitric oxide production, particularly in early stages of disease development. Actarit also alters immunological signaling and symptoms in experimental autoimmune encephalomyelitis, an animal model of multiple sclerosis.
| Cas No. | 18699-02-0 | SDF | |
| 别名 | 阿克他利,4-Acetylaminophenylacetic acid; MS-932 | ||
| Canonical SMILES | CC(NC1=CC=C(CC(O)=O)C=C1)=O | ||
| 分子式 | C10H11NO3 | 分子量 | 193.2 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2)(1:9): 0.1 mg/ml,Ethanol: 3 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.176 mL | 25.8799 mL | 51.7598 mL |
| 5 mM | 1.0352 mL | 5.176 mL | 10.352 mL |
| 10 mM | 0.5176 mL | 2.588 mL | 5.176 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Biosynthesis of Actarit using engineered Escherichia coli
Enzyme Microb Technol 2021 Oct;150:109858.PMID:34489018DOI:10.1016/j.enzmictec.2021.109858.
Actarit is widely regarded as a safe and effective drug for the treatment of rheumatoid arthritis. There is no report on the bioproductin of Actarit so far. In this study, we demonstrated for the first time the development of an artificial Actarit biosynthetic pathway in Escherichia coli. First, 4-aminophenylacetic acid is selected as precursor substrates for the production of Actarit. Second, an N-acetyltransferase that can efficiently catalyse the esterification of acetyl-CoA and 4-aminophenylacetic acid to form Actarit was discovered. Subsequently, an engineered E. coli that allows production of Actarit from simple carbon sources was established. Finally, we further increased the production of Actarit to 206 ± 16.9 mg/L by overexpression of shikimate dehydrogenase ydiB and shikimate kinase aroK.
Injectable actarit-loaded solid lipid nanoparticles as passive targeting therapeutic agents for rheumatoid arthritis
Int J Pharm 2008 Mar 20;352(1-2):273-9.PMID:18054182DOI:10.1016/j.ijpharm.2007.10.014.
This work systematically studied the intravenous injection formulation of solid lipid nanoparticles (SLNs) loaded with Actarit, a poor water soluble anti-rheumatic drug. The goal of this study was to design passive targeting nanoparticles which could improve therapeutic efficacy and reduce side-effects such as nephrotoxicity and gastrointestinal disorders commonly associated with oral formulations of Actarit. Based on the optimized results of single-factor and orthogonal design, actarit-loaded SLNs were prepared by a modified solvent diffusion-evaporation method. The formulated SLNs were found to be relatively uniform in size (241+/-23 nm) with a negative zeta potential (-17.14+/-1.6 mV). The average drug entrapment efficiency and loading were (50.87+/-0.25)% and (8.48+/-0.14)%, respectively. The actarit-loaded SLNs exhibited a longer mean retention time in vivo (t(1/2(beta)), 9.373 h; MRT, 13.53 h) compared with the Actarit 50% propylene glycol solution (t(1/2(ke)), 0.917 h; MRT, 1.323 h) after intravenous injection to New Zealand rabbits. The area under curve of plasma concentration-time (AUC) of actarit-loaded SLNs was 1.88 times greater than that of the Actarit in 50% propylene glycol solution. The overall targeting efficiency (TE(C)) of the actarit-loaded SLNs was enhanced from 6.31% to 16.29% in spleen while the renal distribution of Actarit was significantly reduced as compared to that of the Actarit solution after intravenous administration to mice. These results indicated that injectable actarit-loaded solid lipid nanoparticles were promising passive targeting therapeutic agents for rheumatoid arthritis.
Effect of Actarit on type II collagen-induced arthritis in mice
Arzneimittelforschung 1994 Jan;44(1):64-8.PMID:8135880doi
The effect of Actarit (MS-932, CAS 18699-02-0), an antirheumatic drug, on type II collagen (CII)-induced arthritis in DBA/1J mice was studied. Mice were immunized twice with bovine CII, Actarit being given orally once a day for 35 days after the 1st immunization. Clinical assessment showed that Actarit had no effect on the incidence or day of onset of arthritis but that it lowered the arthritis score dose-dependently. Radiography showed that Actarit reduced new bone formation in the limbs, and a histopathologic examination showed that it reduced synovitis, erosion of cartilage and bone destruction. Actarit suppressed the delayed-type mouse ear skin reaction to CII but had no effect on the level of serum anti-CII antibodies. These results suggest that Actarit inhibits the development of CII-induced arthritis in mice by suppressing delayed-type hypersensitivity to CII.
Double-layered osmotic pump controlled release tablets of Actarit: In vitro and in vivo evaluation
Asian J Pharm Sci 2019 May;14(3):340-348.PMID:32104464DOI:10.1016/j.ajps.2018.05.009.
The aim of the study was to develop Actarit double-layered osmotic pump tablets to overcome the weak points of Actarit common tablets, such as short half-life and large plasma concentration fluctuations. Single factor experiment and orthogonal test were applied to optimize the formulation; the pharmacokinetic study was performed in beagle dogs adopting Actarit common tablets as reference tablets. The optimal formulation was as follows: drug layer: 150 mg Actarit, 240 mg PEO-N80, 50 mg NaCl; push layer: 140 mg PEO-WSR303, 20 mg NaCl; coating solution: 30 g cellulose acetate and 6 g PEG 4000 in 1000 ml 94% acetone solution, 60 mg coating weight gain. The pharmacokinetic study showed that T max was prolonged by the contrast of commercial common tablets with constant drug release rate, but the bioavailability was equivalent. And a good in vivo-in vitro correlation of the Actarit osmotic pump tablets was also established. The designed Actarit osmotic pump tablets can be applied for rheumatoid arthritis, proposing a promising replacement for the marked common products.
Effects of Actarit on synovial cell functions in patients with rheumatoid arthritis
J Rheumatol 1999 Jan;26(1):25-33.PMID:9918236doi
Objective: Actarit (4-acetylaminophenylacetic acid), developed in Japan, has been shown to be effective for suppressing disease activity of rheumatoid arthritis (RA). We analyzed effects of Actarit on synovial cell functions in patients with RA for insight into the clinical application of this medication. Methods: RA primary synovial cells were co-cultured with Actarit at 10(-4)-10(-7) M. Their subsequent proliferative responses and proinflammatory cytokine and matrix metalloproteinase (MMP) production at the mRNA and protein levels were measured. Effects of Actarit on adhesion molecule expression were analyzed by immunofluorescence flow cytometry and cell-cell binding assay. Results: Spontaneous tumor necrosis factor-alpha and interleukin 1beta secretion by primary synovial cells of patients with RA was reduced by Actarit at therapeutic concentrations (10(-5)-10(-6) M). In contrast, Actarit also suppressed MMP-1 production by the primary synovial cells. In addition, Actarit down-regulates CD44 and intercellular adhesion molecule 1 expression on fibroblast-like synovial cell lines, and very late antigen 4 expression on CD14+ macrophage-like synovial cells resulted in the inhibition of lymphocyte adhesion to RA synovial cells. Conclusion: The results suggest that Actarit acts on RA synovial cells to reduce cell-cell interactions with autologous synovium infiltrating lymphocytes and to inhibit proinflammatory cytokine and MMP production, leading to amelioration of symptoms of RA.