|(E)-5-((4-((2-羧基乙基)氨甲酰基)苯基)二氮基)-2-羟基苯甲酸二钠盐二水合物|CsnPharm

CAS No.: 150399-21-6

Balsalazide sodium hydrate/巴柳氮钠水合物 Catalog No. CSN15925

Synonyms: Balsalazide disodium dihydrate;Balsalazide Disodium;balsalazide

Balsalazide Disodium is an anti-inflammatory compound used in the treatment of Inflammatory Bowel Disease.

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生物活性

描述Balsalazide disodium (BSZ) is a colon-specific prodrug of the salicylate, 5-aminosalicylic acid^[3]. It has a variety of biological activities including promoting apoptosis, anti‐inflammatory, and anti‐tumor effects^[4]. ¬¬¬A preliminary mechanistic study in cultured human colon cancer cells showed that BSZ inhibited colon cancer cell proliferation in vitro^[3]. In the murine azoxymethane (AOM)/dextran sodium sulfate (DSS) model, the number of F4/80-positive macrophages was significantly lower in the BSZ-treated groups compared with the CAC (colitis-associated carcinogenesis) group (P < 0.05). At the endpoint, the total numbers of tumors in the BSZ-treated groups were significantly low compared with the CAC group (P < 0.05), and the BSZ-treated groups had significantly lower F4/80-positive macrophages in the tumor stroma (P < 0.01). The protein production of macrophage inflammatory protein 1β, monocyte chemoattractant protein-1, interleukin (IL)-6, and IL-10 in the colon tissues decreased in concordance with the plasma concentrations of the cytokines (P < 0.05). The BSZ-treated groups revealed lower expression of p-STAT3 compared with the CAC group. These results revealed that BSZ have chemopreventive effects against CAC through IL-6/STAT3 suppression^[4]. BSZ treatment of AOM-injected rats reduced ACF (aberrant crypt foci) formation in a dose-dependent manner by 60% with the greatest effect observed on ACF with 4 or more crypts. In B6-Min/+ mice, a dose-dependent reduction of intestinal tumor number was observed which reached 80% in the distal small intestine and colon^[3].
参考文献

[1] Wiggins JB, Rajapakse R. Balsalazide: a novel 5-aminosalicylate prodrug for the treatment of active ulcerative colitis. Expert Opin Drug Metab Toxicol. 2009 Oct;5(10):1279-84.
[2] Kruis W, Schreiber S, et al. Low dose balsalazide (1.5 g twice daily) and mesalazine (0.5 g three times daily) maintained remission of ulcerative colitis but high dose balsalazide (3.0 g twice daily) was superior in preventing relapses. Gut. 2001 Dec;49(6):783-9.
[3] MacGregor DJ, Kim YS, Sleisenger MH, Johnson LK. Chemoprevention of colon cancer carcinogenesis by balsalazide: inhibition of azoxymethane-induced aberrant crypt formation in the rat colon and intestinal tumor formation in the B6-Min/+ mouse. Int J Oncol. 2000 Jul;17(1):173-9. doi: 10.3892/ijo.17.1.173. PMID:10853036.
[4] Do EJ, Hwang SW, Kim SY, Ryu YM, Cho EA, Chung EJ, Park S, Lee HJ, Byeon JS, Ye BD, Yang DH, Park SH, Yang SK, Kim JH, Myung SJ. Suppression of colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway by balsalazide and VSL#3. J Gastroenterol Hepatol. 2016 Aug;31(8):1453-61. doi: 10.1111/jgh.13280. PMID: 26711554.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2867 mL
- 11.4335 mL
- 22.8671 mL
- 5 mM
- 0.4573 mL
- 2.2867 mL
- 4.5734 mL
- 10 mM
- 0.2287 mL
- 1.1434 mL
- 2.2867 mL

技术信息

CAS号

150399-21-6

储存条件

粉末: Keep in dark place,Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H17N3Na2O8

运输

蓝冰

分子量

437.31

别名

Balsalazide disodium dihydrate;Balsalazide Disodium;balsalazide;balsalazine;BX-661A;Colazal;Colazide;巴柳氮钠水合物

溶解度

DMSO	135.0 mg/mL (308.7 mM) warming
Water	110.0 mg/mL (251.5 mM) warming

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Balsalazide sodium hydrate/巴柳氮钠水合物 Catalog No. CSN15925

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