Balsalazide sodium hydrate

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Chemical Structure| 150399-21-6 同义名 : 巴柳氮钠 ;Balsalazide disodium dihydrate; Balsalazide disodium
CAS号 : 150399-21-6
货号 : A639284
分子式 : C17H17N3Na2O8
纯度 : 99%+
分子量 : 437.312
MDL号 : MFCD01631117
存储条件:

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 120 mg/mL(274.4 mM),配合低频超声助溶,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

H2O: 100 mg/mL(228.67 mM),配合低频超声助溶

动物实验配方:
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.43mL

2.29mL

1.14mL

22.87mL

4.57mL

2.29mL

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.