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Sulfasalazine Sale

(Synonyms: 柳氮磺吡啶; NSC 667219) 目录号 : GC16868

Sulfasalazine是一种磺胺类药物。

Sulfasalazine Chemical Structure

Cas No.:599-79-1

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10mM (in 1mL DMSO)
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500mg
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5g
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Description

Sulfasalazine is a sulfonamide drug [1]. Sulfasalazine can inhibit the NF-κB pathway and reduce cytokine release, thereby regulating immune responses [2]. Sulfasalazine is commonly used to treat inflammatory bowel disease and rheumatoid arthritis [3-4].

In Jurkat T-lymphocytes, Sulfasalazine (0.2mM, 0.5mM, 1mM, 2mM; 24h) induces cell apoptosis [5]. In endothelial cells, Sulfasalazine (0.125mM, 24h) inhibits tritiated thymidine incorporation and cell proliferation [6]. In RBL5 cells, Sulfasalazine (1.25mM, 24h) inhibits NF-κB/Rel activation in mouse T lymphocytes [7].

In ICR mice, Sulfasalazine (250mg/kg, 500mg/kg, 1000mg/kg; po; 4 weeks) significantly increased serum levels of ALT, ALP and TBIL [8]. In DSS-Induced ulcerative colitis mice, Sulfasalazine (30mg/kg, 60mg/kg; ip; 7d) can inhibit colon length and mucosal inflammatory infiltration [9]. In middle cerebral artery occlusion mice, Sulfasalazine (5mg/kg, 10mg/kg; iv; single injection) could reduce the infarct size and improve neuro-motor function [10].

References:
[1]. Goldman P, Peppercorn MA. Sulfasalazine. New England Journal of Medicine. 1975 Jul 3; 293(1): 20-23.
[2]. Wahl C, Liptay S, Adler G, et al. Sulfasalazine: a potent and specific inhibitor of nuclear factor kappa B. The Journal of clinical investigation. 1998 Mar 1; 101(5): 1163-1174.
[3]. Peppercorn MA. Sulfasalazine: pharmacology, clinical use, toxicity, and related new drug development. Annals of Internal Medicine. 1984 Sep 1; 101(3): 377-386.
[4]. Plosker GL, Croom KF. Sulfasalazine: a review of its use in the management of rheumatoid arthritis. Drugs. 2005 Sep; 65: 1825-1849.
[5]. Liptay S, Fulda S, Schanbacher M, et al. Molecular mechanisms of sulfasalazine‐induced T‐cell apoptosis. British Journal of Pharmacology. 2002 Nov; 137(5): 608-620.
[6]. Sharon P, Drab EA, Linder JS, et al. The effect of sulfasalazine on bovine endothelial cell proliferation and cell cycle phase distribution: comparison with olsalazine, 5-aminosalicylic acid, and sulfapyridine. The Journal of laboratory and clinical medicine. 1992 Jan 1; 119(1): 99-107.
[7]. Liptay S, Bachem M, Hacker G, et al. Inhibition of nuclear factor kappa B and induction of apoptosis in T‐lymphocytes by sulfasalazine. British journal of pharmacology. 1999 Dec; 128(7): 1361-1369.
[8]. Li YC, Shen JD, Lu SF, et al. Transcriptomic analysis reveals the mechanism of sulfasalazine-induced liver injury in mice. Toxicology Letters. 2020 Mar 15; 321: 12-20.
[9]. Shin MR, Kim KJ, Kim SH, et al. Comparative Evaluation between Sulfasalazine Alone and in Combination with Herbal Medicine on DSS‐Induced Ulcerative Colitis Mice. BioMed Research International. 2017; 2017(1): 6742652.
[10]. Li X, Ding H, Jing J, et al. Sulfasalazine improves neuronal function in mice with ischemic stroke by inhibiting the STING/NF-κB pathway. Naunyn-Schmiedeberg's Archives of Pharmacology. 2025 May; 398(5): 5797-5810.

Sulfasalazine是一种磺胺类药物 [1]。Sulfasalazine可以抑制NF-κB通路并减少细胞因子释放,从而调节免疫反应 [2]。Sulfasalazine常用于治疗炎症性肠病和类风湿性关节炎 [3-4]

在Jurkat T淋巴细胞中,Sulfasalazine(0.2mM、0.5mM、1mM、2mM;24h)诱导细胞凋亡 [5]。在内皮细胞中,Sulfasalazine(0.125mM;24h)抑制氚化胸苷的掺入和细胞增殖 [6]。在RBL5细胞中,Sulfasalazine(1.25mM;24h)抑制小鼠T淋巴细胞中的NF-κB/Rel活化 [7]

在ICR小鼠中,Sulfasalazine(250mg/kg、500mg/kg、1000mg/kg;po;4周)显著升高血清ALT、ALP和TBIL水平 [8]。在DSS诱发的溃疡性结肠炎小鼠中,Sulfasalazine(30mg/kg、60mg/kg;ip;7d)可抑制结肠长度和粘膜炎症浸润 [9]。在大脑中动脉闭塞小鼠中,Sulfasalazine(5mg/kg、10mg/kg;iv;单次注射)可缩小梗死面积并改善神经运动功能 [10]

实验参考方法

Cell experiment [1]:

Cell lines

Jurkat T-lymphocytes

Preparation Method

Jurkat T-lymphocytes were grown under standard conditions in RPMI 1640 medium supplemented with 100U/mL penicillin, 100μg/mL streptomycin, 2mM glutamine, and 10% FCS. Sulfasalazine was freshly dissolved in the medium and added to the culture at the indicated concentrations and times.

Reaction Conditions

0.2mM, 0.5mM, 1mM, 2mM; 24h

Applications

Sulfasalazine induces apoptosis in human Jurkat T-lymphocytes.
Animal experiment [2]:

Animal models

ICR mice

Preparation Method

Forty ICR mice were randomly divided into four experimental groups (n = 10): control group and Sulfasalazine (SASP) groups (250mg/kg, 500mg/kg, 1000mg/kg). SASP (98% of purity) was dissolved in 0.1% dimethyl sulfoxide (DMSO) and were administered by oral gavage in a volume of 10mL/kg for 4 weeks. Control group received equal volume of 0.1% DMSO.

Dosage form

250mg/kg, 500mg/kg, 1000mg/kg; po; 4 weeks

Applications

Sulfasalazine significantly increased serum levels of ALT, ALP and TBIL.

References:
[1]. Liptay S, Fulda S, Schanbacher M, et al. Molecular mechanisms of sulfasalazinen-induced T-cell apoptosis. British Journal of Pharmacology. 2002 Nov; 137(5): 608-620.
[2]. Li YC, Shen JD, Lu SF, et al. Transcriptomic analysis reveals the mechanism of sulfasalazine-induced liver injury in mice. Toxicology Letters. 2020 Mar 15; 321: 12-20.

化学性质

Cas No. 599-79-1 SDF
别名 柳氮磺吡啶; NSC 667219
化学名 (3Z)-6-oxo-3-[[4-(pyridin-2-ylsulfamoyl)phenyl]hydrazinylidene]cyclohexa-1,4-diene-1-carboxylic acid
Canonical SMILES C1=CC=NC(=C1)NS(=O)(=O)C2=CC=C(C=C2)NN=C3C=CC(=O)C(=C3)C(=O)O
分子式 C18H14N4O5S 分子量 398.39
溶解度 ≥ 17.7 mg/mL in DMSO 储存条件 Store at RT
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1 mg 5 mg 10 mg
1 mM 2.5101 mL 12.5505 mL 25.101 mL
5 mM 0.502 mL 2.5101 mL 5.0202 mL
10 mM 0.251 mL 1.2551 mL 2.5101 mL
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