货号:A105320 同义名: 5-氨基-2-羟基苯甲酸 / Mesalamine;5-ASA
5-Aminosalicylic Acid is a potent inhibitor of interleukin 1 β production used to treat inflammatory bowel disease.
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产品名称 | NF-κB ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
PDTC ammonium | ✔ | 98% | |||||||||||||||||
QNZ |
++++
NF-κB, IC50: 11 nM |
99%+ | |||||||||||||||||
Sodium 4-Aminosalicylate Dihydrate | ✔ | 98% | |||||||||||||||||
Sodium Salicylate | ✔ | 95% | |||||||||||||||||
Parthenolide | ✔ | p53 | 97% HPLC | ||||||||||||||||
JSH-23 |
+
NF-κB, IC50: 7.1 μM |
98% | |||||||||||||||||
Phenethyl caffeate | ✔ | 98% | |||||||||||||||||
Andrographolide | ✔ | 98+% | |||||||||||||||||
Curcumin | ✔ | Nrf2,HDAC | 98% | ||||||||||||||||
SC75741 |
+++
NF-κB, EC50: 200 nM |
99%+ | |||||||||||||||||
CBL0137 HCl |
++
NF-κB, EC50: 0.47 μM |
p53 | 99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
描述 | F-5-Aminosalicylic acid (5-ASA) is a specific agonist for PPARγ, and only PPARγ but not PPARα or PPARδ induces p65 degradation. 5-Aminosalicylic acid induces degradation of p65 protein indicative of PPARγ's E3 ubiquitin ligase activity. 5-Aminosalicylic acid blocks NF-κB in intestinal epithelial cells (IECs) through inhibition of PAK1[3]. Pretreatment with 5-Aminosalicylic acid (5-ASA) or Nimesulide at different concentration (10-1000 μmol/L) for 12-96 h, inhibits the growth of HT-29 colon carcinoma cells in a dose and time-dependent manner. Combined 5-Aminosalicylic acid (final concentration 100 μM) and Nimesulide (final concentration 10-1000 μM) inhibits the proliferation of HT-29 colon carcinoma cells in a dose-dependent manner, being more potent than corresponding dose of Nimesulide. In A/JOlaHsd mice, 5-ASA suppressed colon carcinogenesis by decreasing the number of aberrant crypt foci (75%) and aberrant crypts (22%) induced by AOM (azoxymethane) treatment with an absence of 5-ASA response after GW9662 administration[4]. Pretreatment with 5-ASA or nimesulide at the concentration of 10-1000 micromol/L inhibited proliferation of HT-29 colon carcinoma cells in a dose-dependent manner in vitro. The inhibition rate of HT-29 colon carcinoma cell proliferation was also increased when pretreated with 5-ASA (100 micromol/L) or nimesulide (100 micromol/L) for 12-96 h, which showed an obvious time-effect relationship. 5-ASA and nimesulide may inhibit the proliferation of HT-29 colon carcinoma cells and coadministration of these agents may have additional chemopreventive potential[5]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT00746447 | Colitis, Ulcerative ... 展开 >> Recurrence 收起 << | Phase 3 | Completed | - | Germany ... 展开 >> Evangelisches Krankenhaus Kalk, Medical Dept. Cologne, Germany, 51103 收起 << |
NCT01699438 | Irritable Bowel Syndrome | Phase 2 | Completed | - | Sweden ... 展开 >> Sahlgrenska University Hospital Göteborg, Sweden Karolinska University Hospital Huddinge, Sweden Norrland's University Hospital Umeå, Sweden 收起 << |
NCT01257399 | Ulcerative Colitis in Remissio... 展开 >>n 收起 << | Phase 3 | Completed | - | China ... 展开 >> Shanghai Hospital Shanghai, China 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
6.53mL 1.31mL 0.65mL |
32.65mL 6.53mL 3.27mL |
65.30mL 13.06mL 6.53mL |
CAS号 | 89-57-6 |
分子式 | C7H7NO3 |
分子量 | 153.135 |
别名 | 5-氨基-2-羟基苯甲酸 ;Mesalamine;5-ASA;MAX-002;AJG-501;Z-206;Asacol;Mesalazine |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Room temperature |
溶解度 |
DMSO: 65 mg/mL(424.46 mM),配合低频超声,并水浴加热至45℃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 |