5-Aminosalicylic Acid

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Chemical Structure| 89-57-6 同义名 : 5-氨基-2-羟基苯甲酸 ;Mesalamine;5-ASA;MAX-002;AJG-501;Z-206;Asacol;Mesalazine
CAS号 : 89-57-6
货号 : A105320
分子式 : C7H7NO3
纯度 : 98%
分子量 : 153.135
MDL号 : -
存储条件:

Pure form Keep in dark place,Inert atmosphere,Room temperature

In solvent -20°C:3-6个月-80°C:12个月

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:
生物活性
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].
临床研究
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 <<
实验方案
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

参考文献

[1]Khare V, Lyakhovich A, et al. Mesalamine modulates intercellular adhesion through inhibition of p-21 activated kinase-1. Biochem Pharmacol. 2013 Jan 15;85(2):234-44.

[2]Egan LJ, Mays DC, et al. Inhibition of interleukin-1-stimulated NF-kappaB RelA/p65 phosphorylation by mesalamine is accompanied by decreased transcriptional activity. J Biol Chem. 1999 Sep 10;274(37):26448-53.

[3]Dammann K, Khare V, Lang M, Claudel T, Harpain F, Granofszky N, Evstatiev R, Williams JM, Pritchard DM, Watson A, Gasche C. PAK1 modulates a PPARγ/NF-κB cascade in intestinal inflammation. Biochim Biophys Acta. 2015 Oct;1853(10 Pt A):2349-60

[4]Rousseaux C, El-Jamal N, Fumery M, Dubuquoy C, Romano O, Chatelain D, Langlois A, Bertin B, Buob D, Colombel JF, Cortot A, Desreumaux P, Dubuquoy L. The 5-aminosalicylic acid antineoplastic effect in the intestine is mediated by PPARγ. Carcinogenesis. 2013 Nov;34(11):2580-6

[5]Fang HM, Mei Q, Xu JM, Ma WJ. 5-aminosalicylic acid in combination with nimesulide inhibits proliferation of colon carcinoma cells in vitro. World J Gastroenterol. 2007 May 28;13(20):2872-7