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-β 和 COX-2 的抑制剂。Sulfasalazine 可诱导铁死亡、凋亡和自噬。
Sulfasalazine Chemical Structure
CAS: 599-79-1
产品质控
批次：
纯度：
99.86%
99.86
Sulfasalazine相关产品
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-β 和 COX-2 的抑制剂。Sulfasalazine 可诱导铁死亡、凋亡和自噬。 | |||
|---|---|---|---|---|
| 靶点 |
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| 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] |
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|---|---|---|---|---|
| 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) | |||
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体外溶解度 |
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 |
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体内溶解度 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
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
只
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，注：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：取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：取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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