Iguratimod

产品说明书

Print
Chemical Structure| 123663-49-0 同义名 : T614; IGU; N7methanesulfonamido4oxo6(phenoxy)chromen3ylformamide
CAS号 : 123663-49-0
货号 : A178057
分子式 : C17H14N2O6S
纯度 : 98%
分子量 : 374.37
MDL号 : MFCD00882374
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(93.49 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Iguratimod (T-614) is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod (0.1, 1, 10 μg/mL) inhibits bradykinin-stimulated PGE2 (prostaglandin E2) release from fibroblasts. Iguratimod suppresses the COX activity from bradykinin stimulated fibroblasts in a concentration-dependent manner, with an IC50 of 48 μg/mL. Iguratimod (10 and 30 μg/mL) also dose-dependently inhibits COX-2 mRNA levels[3]. Mechanical paw withdrawal thresholds and the expression levels of pERK (phosphorylated extracellular signal-related kinase) and c-Fos declined in a dose-dependent manner in rats treated with iguratimod, and bone destruction severity was also reduced[4]. In addition, Iguratimod potently inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM. Iguratimod is synergetic with glucocorticoids in vitro. Iguratimod (20 mg/kg i.p.) shows significantly increased survival in BALB/c mice that are vulnerable to endotoxemia, and attenuates TNFα release measured in serum isolated 90 min post-LPS administration in wild-type C57BL/6 mice[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.67mL

0.53mL

0.27mL

13.36mL

2.67mL

1.34mL

26.71mL

5.34mL

2.67mL
参考文献

[1]Zhou T, Ding L, et al. Determination of iguratimod in rat plasma by high performance liquid chromatography: method and application. Biomed Chromatogr. 2008 Mar;22(3):260-4.

[2]Tanaka K, Urata N, et al. Effect of iguratimod and other anti-rheumatic drugs on adenocarcinoma colon 26-induced cachexia in mice. Inflamm Res. 2007 Jan;56(1):17-23.

[3]Tanaka K, Kawasaki H, Kurata K, Aikawa Y, Tsukamoto Y, Inaba T. T-614, a novel antirheumatic drug, inhibits both the activity and induction of cyclooxygenase-2 (COX-2) in cultured fibroblasts. Jpn J Pharmacol. 1995;67(4):305-314

[4]Sun Y, Wu YX, Zhang P, Peng G, Yu SY. Anti-rheumatic drug iguratimod protects against cancer-induced bone pain and bone destruction in a rat model. Oncol Lett. 2017;13(6):4849-4856

[5]Bloom J, Metz C, Nalawade S, et al. Identification of Iguratimod as an Inhibitor of Macrophage Migration Inhibitory Factor (MIF) with Steroid-sparing Potential. J Biol Chem. 2016;291(51):26502-26514