Iguratimod
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
对于IL-6产生,IC50值为2.0 μg/ml(肝细胞刺激活性)和6.6 μg/ml(免疫反应)。
Iguratimod是4H-1-苯并吡喃-4-酮系列之一,具有高效的抗炎、退热和止痛活性。Iguratimod也能抑制白介素-1(IL-1)、IL-6、IL-8和肿瘤坏死因子的产生。
体外实验:Iguratimod以剂量依赖的方式(0.3-30 μg/ml)抑制脂多糖(LPS)刺激的人单核细胞系免疫反应性IL-1β的分泌。Northern印记分析LPS刺激的THP-1细胞表明Iguratimod通过抑制IL-1β mRNA表达从而抑制IL-1的产生[1]。
体内试验:给予Iguratimod并不抑制肿瘤生长,但会减轻恶性病症状。而且,Iguratimod降低了血清中IL-6的水平,也降低了其基因在肿瘤组织中的表达。另外,外源性IL-6并不会抵消Iguratimod的抑制效应[2]。
临床试验:日本394例类风湿性关节炎病人为期52周的临床研究以评估此药物的长期安全性。按前四周每天25 mg、后48周每天50 mg的剂量口服Iguratimod。100周内不良事件的积累发生率为97.6%。不良反应的积累发生率为65.3%;不良症状和体征占反应的33.2%,异常的实验数据变化占50.4%[3]
参考文献:
[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.
Storage | Store at -20°C |
M.Wt | 374.37 |
Cas No. | 123663-49-0 |
Formula | C17H14N2O6S |
Synonyms | T 614;T-614;T614 |
Solubility | Soluble in DMSO |
Chemical Name | N-[7-(methanesulfonamido)-4-oxo-6-phenoxychromen-3-yl]formamide |
SDF | Download SDF |
Canonical SMILES | CS(=O)(=O)NC1=C(C=C2C(=C1)OC=C(C2=O)NC=O)OC3=CC=CC=C3 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
Description | Iguratimod(T-614)是环加氧酶-2(COX-2)的选择性抑制剂,抑制IL-1、IL-6、IL-8和肿瘤坏死因子的产生。 | |||||
靶点 | COX-2 | |||||
IC50 |