CAS NO: | 89-57-6 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
生物活性 | 5-Aminosalicylic acid (Mesalamine) acts as a specificPPARγagonist and also inhibitsp21-activated kinase 1(PAK1) andNF-κB. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | 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 also inhibits PAK1 at the mRNA level which is suggestive of an additional mechanism independent of PPARγ ligand activation. 5-Aminosalicylic acid blocks NF-κB in intestinal epithelial cells (IECs) through inhibition of PAK1[1]. 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. However, the suppression of 5-Aminosalicylic acid or Nimesulide has no statistical significance. The growth of HT-29 colon carcinoma cells is inhibited dose-dependently when pretreated with different doses of combined 5-Aminosalicylic acid and Nimesulide. 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. Similarly, combined Nimesulide (final concentration 100 μM) and 5-Aminosalicylic acid (final concentration 10-1000 μM) also inhibits the proliferation of these cells dose-dependently, being more potent than corresponding dose of 5-Aminosalicylic acid[2]. | ||||||||||||||||
体内研究 (In Vivo) | 5-Aminosalicylic acid (5-ASA) has an antineoplastic effect in a xenograft tumor model. To evaluate the in vivo antineoplasic effect of 5-Aminosalicylic acid, SCID mice engrafted with HT-29 colon cancer cells are treated daily for 21 consecutive days with 5-Aminosalicylic acid at 50 mM. At the end of the treatment, a reduction of 80-86% of tumor weight and volume is observed in SCID mice receiving 5-Aminosalicylic acid compared with control mice or mice treated with GW9662 alone. The antineoplastic effect of 5-Aminosalicylic acid is already detectable after 10 days of 5-Aminosalicylic acid treatment. Similar results are obtained with mice treated with 5-Aminosalicylic acid at 5 mM. Antitumorigenic effect of 5-Aminosalicylic acid is completely abolished at 21 days by simultaneous intraperitoneal administration of GW9662. Thus, the observed antineoplastic effect of 5-Aminosalicylic acid is at least partially dependent on PPARγ[3]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 153.14 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C7H7NO3 | ||||||||||||||||
CAS 号 | 89-57-6 | ||||||||||||||||
中文名称 | 美沙拉嗪;5-氨基水杨酸 | ||||||||||||||||
结构分类 |
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运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) | ||||||||||||||||
溶解性数据 | In Vitro: DMSO : ≥ 6 mg/mL(39.18 mM) H2O : 2 mg/mL(13.06 mM;ultrasonic and warming and heat to 60℃) *"≥" means soluble, but saturation unknown. 配制储备液
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