Sulfasalazine

别名: NSC 667219, Sulphasalazine 中文名称:柳氮磺吡啶

Sulfasalazine是一种磺胺剂,是Mesalazine的衍生物,主要用作抗炎剂。Sulfasalazine 是一种有效的、特异性的 nuclear factor kappa B (NF-κB)TGF-βCOX-2 的抑制剂。Sulfasalazine 可诱导铁死亡、凋亡和自噬。

Sulfasalazine Chemical Structure

Sulfasalazine Chemical Structure

CAS: 599-79-1

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 647.05 现货
500mg RMB 573.83 现货
1g RMB 892.75 现货
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产品质控

批次: 纯度: 99.86%
99.21

Sulfasalazine相关产品

Immunology & Inflammation related抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
HepG2 Function assay 1 hr Inhibition of NF-kappaB activation expressed in TNFalpha-stimulated human HepG2 cells co-transfected with PPRE-Luc plasmid pretreated for 1 hr before TNFalpha challenge measured after 24 hrs by luciferase reporter gene assay, IC50=0.9μM 21889336
HepG2 Function assay 1 hr Inhibition of TNF-alpha-induced NFkappaB activation in human HepG2 cells after 1 hr by luciferase reporter assay, IC50=0.9μM 21870831
HepG2 Function assay 1 hr Inhibition of TNFalpha-induced NFkappaB transcriptional activity in human HepG2 cells pretreated for 1 hr before TNFalpha challenge by luciferase reporter gene analysis, IC50=0.9μM 22381047
HepG2 Function assay 1 hr Inhibition of NF-kappaB expressed in human HepG2 cells assessed as inhibition of TNFalpha-induced luciferase activity preincubated for 1 hr followed by TNFalpha challenge measured after 1 hr by reporter gene assay, IC50=0.9μM 23031596
HepG2 Function assay 1 hr Inhibition of TNF-alpha-induced NF-kappaB transcriptional activation in human HepG2 cells preincubated for 1 hr followed by TNF-alpha challenge measured after 1 hr by luciferase reporter gene assay, IC50=0.9μM 24314396
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, Ki=3μM 22541068
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting, IC50=3μM 22541068
U2OS Function assay 10 mins Inhibition of HA-tagged human NTCP expressed in human U2OS cells assessed as reduction in [14C]taurocholate uptake preincubated for 10 mins followed by [14C] taurocholate addition and further incubation for 10 mins by scintillation counting method, IC50=9.6μM 31439379
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, Ki=11μM 22541068
HEK293 Flp-In Function assay 5 mins Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting, IC50=12μM 22541068
U87 Function assay 15 mins Inhibition of xc-cystine-glutamate antiporter-mediated cystine uptake in human U87 cells using L-[14C]cystine as substrate after 15 mins by liquid scintillation counting, IC50=30μM 21889337
HEK293 Flp-In Function assay Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, Ki=0.53μM 22541068
HEK293 Flp-In Function assay Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting, IC50=0.56μM 22541068
点击查看更多细胞系数据

生物活性

产品描述 Sulfasalazine是一种磺胺剂,是Mesalazine的衍生物,主要用作抗炎剂。Sulfasalazine 是一种有效的、特异性的 nuclear factor kappa B (NF-κB)TGF-βCOX-2 的抑制剂。Sulfasalazine 可诱导铁死亡、凋亡和自噬。
靶点
NF-κB [4] COX-2 [4] TGF-β [4]
体外研究(In Vitro)
体外研究活性

Sulfasalazin,像甲氨蝶呤一样,增强了发炎部位释放腺苷,并且腺苷通过炎症细胞的A2受体减少炎症。[1] Sulfasalazin处理4小时抑制κB依赖性转录,IC 50值大约为0.625 mM。Sulfasalazin(2.5 mM)以剂量和时间依赖性导致T淋巴细胞的细胞死亡。Sulfasalazin,但不是5ASA或者sulfapyridine,强力抑制NF-κB活化并有力地诱导T淋巴细胞的细胞凋亡。[2] Sulfasalazin通过结肠细菌裂解成sulfapyridine和5-氨基水杨酸(5-ASA;mesalamine),而后者也抑制NF-κB活性。Sulfasalazin但不是其裂解形式5-ASA剂量依赖性抑制胶质瘤的增长,这种效果是完全归因于胱氨酸摄取,经由系统x(c)中抑制(- )胱氨酸谷氨酸转运。Sulfasalazin抑制胱氨酸摄入,引起细胞内谷胱甘肽的慢性消耗,从而破坏细胞的氧化还原防御,阻碍肿瘤生长。[3]

体内研究(In Vivo)
体内研究活性

在小鼠气囊模型中,Sulfasalazin显著降低发炎(carrageenan, 2 毫克/毫升)气囊中积累的白细胞的数量。Sulfasalazin处理促进splenocyte 5-aminoimidazole-4-carboxamidoribonucleotide (AICAR)浓度的显著增加,和体外观察到的Sulfasalazin抑制AICAR甲酰基转移酶一致。[1]

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06134388 Recruiting
Metastatic Colorectal Cancer
Tanta University
September 1 2023 Phase 3
NCT03487926 Active not recruiting
Major Depressive Episode|Inflammatory Bowel Diseases
Centre for Addiction and Mental Health|McMaster University
September 14 2022 --
NCT04720183 Completed
Healthy
Galapagos NV
January 11 2021 Phase 1
NCT01577966 Completed
Brain Tumor
University of Alabama at Birmingham
January 2012 Not Applicable

化学信息&溶解度

分子量 398.39 分子式

C18H14N4O5S

CAS号 599-79-1 SDF Download Sulfasalazine SDF Download Sulfasalazine SDF
Smiles C1=CC=NC(=C1)NS(=O)(=O)C2=CC=C(C=C2)N=NC3=CC(=C(C=C3)O)C(=O)O
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 80 mg/mL ( 200.8 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

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