Iguratimod
(Synonyms: 艾拉莫德; T614) 目录号 : GC17419
A DMARD and COX-2 inhibitor
Cas No.:123663-49-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | Briefly, human Raji B cells are plated at a density of 0.5 × 104 cells/well in a 96-well plate and synchronized by incubation for 24 h in RPMI 1640 medium supplemented with 0.1-0.5% FBS. Synchronized cells are pretreated with Iguratimod or vehicle for 30 min prior to stimulation with macrophage migration inhibitory factor (MIF) for 24 h. At 20 h BrdU is added to cells and quantified using a BrdU Cell proliferation assay kit[3]. |
Animal experiment: | Mice[3]Endotoxemia is induced by intraperitoneal injection of LPS from E. coli O111:B4. In BALB/c animals, 5 mg/kg LPS is used as a lethal dose for survival experiments; animals are treated with Iguratimod (20 mg/kg i.p.) 0.5 h prior to LPS, 6 h after LPS, and then once daily for 3 days and monitored for survival over 2 weeks. In C57BL/6 animals, 20 mg/kg LPS is used as non-lethal dose for plasma cytokine experiments; animals are pretreated with Iguratimod (20 mg/kg i.p.) twice, one dose each at 2 and 0.5 h prior to LPS administration, and euthanized at 90 min post-LPS by CO2 asphyxiation with cervical dislocation. Blood is collected by cardiac puncture and allowed to clot 20 min at room temperature and 20 min at 4°C; sera are isolated by centrifugation at 300 × g for 10 min and stored at −20°C for further analysis by TNFα ELISA (1:3 dilution)[3]. |
References: [1]. Tanaka K, et al. T-614, a novel antirheumatic drug, inhibits both the activity and induction of cyclooxygenase-2 (COX-2) in cultured fibroblasts. Jpn J Pharmacol. 1995 Apr;67(4):305-14. | |
IC50: 2.0 (hepatocyte-stimulating activities) and 6.6 μg/ml (immunoreactivities) for IL-6 release.
Iguratimod is one of a series of 4H-1-benzopyran-4-ones which has potent anti-inflammatory, antipyretic and analgesic activity. Iguratimod also inhibits the production of tumour necrosis factor and interleukin-1 (IL-1), IL-6, IL-8.
In vitro: Iguratimod inhibited the release of immunoreactive IL-1 beta from human monocytic cell line stimulated with lipopolysaccharides (LPS) in a dose-dependent manner (0.3-30 μg/ml). Northern blotting analysis using LPS-stimulated THP-1 cells indicated that the inhibitory effect of Iguratimod on IL-1 beta production is caused by the suppression of IL-1 beta mRNA expression [1].
In vivo: Administration of Iguratimod did not inhibit the tumor growth, but resulted in attenuation of cachexia symptoms. Furthermore, Iguratimod decreased the serum levels of IL-6, and also reduced its gene expression in the tumor tissues. In addition, exogenously administered IL-6 nullified the suppressive effect of Iguratimod [2].
Clinical trial: A 52-week clinical study of iguratimod in 394 Japanese patients with rheumatoid arthritis to evaluate the long-term safety of the drug was conducted. Iguratimod was administered orally at a daily dose of 25 mg for the first 4 weeks and 50 mg for the subsequent 48 weeks. The cumulative incidence of adverse events for 100 weeks was 97.6%. The cumulative incidence of adverse reactions was 65.3%; unfavorable symptoms and signs accounted for 33.2% of the reactions, and abnormal laboratory data changes accounted for 50.4% [3].
References:
[1] Tanaka K, Aikawa Y, Kawasaki H, Asaoka K, Inaba T, Yoshida C. Pharmacological studies on 3-formylamino-7-methylsulfonylamino-6-phenoxy-4H-1-benzopyran-4-one (T-614), a novel antiinflammatory agent. 4th communication: inhibitory effect on the production of interleukin-1 and interleukin-6. J Pharmacobiodyn. 1992;15(11):649-55.
[2] Tanaka K, Urata N, Mikami M, Ogasawara M, Matsunaga T, Terashima N, Suzuki H. Effect of iguratimod and other anti-rheumatic drugs on adenocarcinoma colon 26-induced cachexia in mice. Inflamm Res. 2007;56(1):17-23.
[3] Hara M, Abe T, Sugawara S, Mizushima Y, Hoshi K, Irimajiri S, Hashimoto H, Yoshino S, Matsui N, Nobunaga M. Long-term safety study of iguratimod in patients with rheumatoid arthritis. Mod Rheumatol. 2007;17(1):10-6.
| Cas No. | 123663-49-0 | SDF | |
| 别名 | 艾拉莫德; T614 | ||
| 化学名 | N-[7-(methanesulfonamido)-4-oxo-6-phenoxychromen-3-yl]formamide | ||
| Canonical SMILES | CS(=O)(=O)NC1=C(C=C2C(=C1)OC=C(C2=O)NC=O)OC3=CC=CC=C3 | ||
| 分子式 | C17H14N2O6S | 分子量 | 374.37 |
| 溶解度 | DMSO : 50mg/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 | 2.6712 mL | 13.3558 mL | 26.7115 mL |
| 5 mM | 0.5342 mL | 2.6712 mL | 5.3423 mL |
| 10 mM | 0.2671 mL | 1.3356 mL | 2.6712 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，
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2.
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