Mesalamine.|89-57-6|(5-氨基水杨酸; Mesalamine; 5-ASA; Mesalazine)-陌孚医药/Medlife

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Mesalamine. (Synonyms: 5-氨基水杨酸; Mesalamine; 5-ASA; Mesalazine)

目录号: PC11556 纯度: ≥98%

CAS No. :89-57-6

商品编号	规格	价格	会员价	是否有货	数量
PC11556-10g	10g	¥362.60	请登录
PC11556-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥490.00	请登录

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中文名称	Mesalamine.
中文别名	氨水杨酸;5-氨基水杨酸;2-羟基-5-氨基苯甲酸;3-羧基-4-羟基苯胺;间氨基水杨酸;5-氨基-2-羟基苯甲酸;美沙拉秦;马拉沙嗪;美沙拉嗪;5-氨基水杨酸[用于生化研究];5 - 氨基水杨酸标准品;5-Aminosalicylic Acid 5-氨基水杨酸;5-Aminosalicylic Acid [for Biochemical Research] 5-氨基水杨酸[用于生化研究];5-Aminosalicylicacid,certified 标准品;5-氨基水杨酸(美沙拉秦);5-氨基水杨酸（美沙拉嗪）;5-氨基水杨酸及合成技术;ASA氨水杨酸;氨水杨酸(5-氨基水杨酸);马沙拉嗪;马沙拉嗪,5-氨基水杨酸;美沙拉秦系统适用性 EP标准品;美沙拉嗪 EP标准品;美沙拉嗪 USP标准品;美沙拉嗪标准品;美沙拉嗪(5-氨基水杨酸);美沙啦嗪(5-氨基水杨酸);5-氨水杨酸
英文名称	Mesalamine
英文别名	5-Amino-2-hydroxybenzoic acid;IFLAB-BB F1918-0003;BENZOIC ACID, 5-AMINO-2-HYDROXY-;M-AMINOSALICYLIC ACID;MESALAMINE;MESALAZINE;2-HYDROXY-5-AMINOBENZOIC ACID;3-Carboxy-4-hydroxyaniline;5-Aminosalicylic acid;5-AS;5-Aminosalicylic Acid [for Biochemical Research];5-Aminosalicylic Acid (Mesalazine);2-Cyanobenzoic acid;5-AMINO-2-HYDROXYBENZOIC ACID FOR SYNTHESIS;5-Aminosalicglic acid;5-AMINOSALICILIC ACID;5-AMINOSALICYLIC ACID (MESALAZINE);5-AMINOSALICYLIC ACID , CRM STANDARD;5-AMinosalicylic Acid, Purified;5-ASA;Mesalamine (Lialda);Rowasa;Asacol;Pentasa;Claversal;Canasa;Salofalk;Mesasal;Lialda;Fisalamine;Lixacol;Apriso;p-Aminosalicylsaeure;sfRowasa;Mesalazinum;Asacolitin;Mesalazina;5-amino-2-hydroxy-benzoic acid;Asacol HD;Mesalazinum [Latin];5-Amino Salicylic Acid;Mesalamine [USAN];Mesalazina [Spanish];p-Aminosalicylsaeure [German];SALICYLIC ACID, 5-AMI
Cas No.	89-57-6
分子式	C₇H₇NO₃
分子量	153.14
包装储存	4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

生物活性

5-Aminosalicylic acid (Mesalamine) acts as a specific PPARγ agonist and also inhibits p21-activated kinase 1 (PAK1) and NF-κB.

性状

Solid

IC50 & Target[1][2]

PPARγ

PAK1

p65

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 PPARγs 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. 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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

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)

ClinicalTrial

结构分类

Ketones, Aldehydes, Acids

参考文献

[1]. Dammann K, et al. PAK1 modulates a PPARγ/NF-κB cascade in intestinal inflammation. Biochim Biophys Acta. 2015 Oct;1853(10 Pt A):2349-60. [Information]

[2]. Rousseaux C, et al. The 5-aminosalicylic acid antineoplastic effect in the intestine is mediated by PPARγ. Carcinogenesis. 2013 Nov;34(11):2580-6. [Information]

[3]. Fang HM, et al. 5-aminosalicylic acid in combination with Nimesulide inhibits proliferation of colon carcinoma cells 体外研究. World J Gastroenterol. 2007 May 28;13(20):2872-7. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (653.00 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	6.5300 mL	32.6499 mL	65.2997 mL
5 mM	1.3060 mL	6.5300 mL	13.0599 mL
10 mM	0.6530 mL	3.2650 mL	6.5300 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 50% PEG300 50% saline
Solubility: 7.14 mg/mL (46.62 mM); Suspended solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (16.32 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (16.32 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (16.32 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (16.32 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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