柳氮磺胺吡啶, 质子偶联叶酸转运体抑制剂

TGF-β Selective Inhibitors | Activators | Agonists | Modulators
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货号 (SKU) 包装规格 是否现货 价格 数量
S409257-1ml
1ml 现货 Stock Image
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Compound libraries (12332)

基本描述

英文别名 Azulfidine, Salazopyrin, Sulphasalazine | 2-​hydroxy-​5-​[2-​[4-​[(2-​pyridinylamino)​sulfonyl]​phenyl]​diazenyl]​-benzoic acid
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Sulfasalazine (NSC 667219)
生化机理 磺胺嘧啶(Sulfasalazine,NSC 667219,Azulfidine,Salazopyrin,Sulphasalazine)是美沙拉嗪的磺胺衍生物,可作为抗炎药物治疗肠道疾病和类风湿性关节炎。磺胺嘧啶是核因子卡巴 B(NF-κB)、TGF-β 和 COX-2 的强效特异性抑制剂。柳氮磺胺吡啶可诱导铁变态反应、细胞凋亡和自噬。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 质子偶联叶酸转运体抑制剂
产品介绍

Sulfasalazine 是一种磺胺剂,是Mesalazine的衍生物,主要用作抗炎剂。An inhibitor of of GSH-H-transferase and NF-kB activation and an apoptosis inducer

Information

Sulfasalazine (NSC 667219, Azulfidine, Salazopyrin, Sulphasalazine) is a sulfa derivative of mesalazine, used as an anti-inflammatory agent to treat bowel disease and rheumatoid arthritis. Sulfasalazine is a potent and specific inhibitor ofnuclear factor
In vitro

Sulfasalazine, like methotrexate, enhances adenosine release at an inflamed site and that adenosine diminishes inflammation via occupancy of A2 receptors on inflammatory cells. Sulfasalazine treatment for 4 hours inhibits kappaB-dependent transcription with an IC50 value of approximately 0.625 mM. Sulfasalazine (2.5 mM) results in cell death of T-lymphocytes in a dose- and time-dependent manner. Sulfasalazine but not 5ASA or sulfapyridine, strongly inhibits NF-kappaB activation and potently induces apoptosis in T-lymphocytes. Sulfasalazine is cleaved into sulfapyridine and 5-aminosalicylic acid (5-ASA; mesalamine) by colonic bacteria, and the latter, too, is reported to suppress NF-kappaB activity. Sulfasalazine but not its cleaved form 5-ASA causes a dose-dependent inhibition of glioma growth, this effect is entirely attributable to the inhibition of cystine uptake via the system x(c)(-) cystine-glutamate transporter. Sulfasalazine inhibits cystine uptake causing a chronic depletion of intracellular GSH and consequently compromised cellular redox defense which stymied tumor growth.

In vivo

Sulfasalazine markedly decreases the number of leukocytes that accumulated in the inflamed (carrageenan, 2 mg/ml) air pouch in the murine air pouch model of inflammation. Sulfasalazine treatment promotes a marked increase in splenocyte 5-aminoimidazole-4-carboxamidoribonucleotide (AICAR) concentration, which is consistent with the in vitro observation that sulfasalazine inhibits AICAR transformylase.
Cell Data

cell lines:p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines.

Concentrations:Concentrations:

Incubation Time:Incubation Time:

Powder Purity:≥98%

关联靶点(人)

SLC46A1 Tchem 质子偶联叶酸转运体(Proton-coupled folate transporter) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

Canonical SMILES OC(=O)C1=C(O)C=CC(=C1)N=NC2=CC=C(C=C2)[S](=O)(=O)NC3=CC=CC=N3
分子量 398.39

化学和物理性质

溶解性 Solubility (25°C) In vitro DMSO: 47 mg/mL (197.24 mM);    

安全和危险性(GHS)

技术规格说明书

Record the entire process by video Conform
Concentration(Compounding value) 9.0-11.0(mmol/L)

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

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