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Sulfasalazine
僅限科研使用
Sulfasalazine
別名: NSC 667219, Sulphasalazine 中文名稱：柳氮磺吡啶
Sulfasalazine是一種磺胺劑，是Mesalazine的衍生物，主要用作抗炎劑。Sulfasalazine 是一種有效的、特異性的 nuclear factor kappa B (NF-κB)、TGF-β 和 COX-2 的抑制劑。Sulfasalazine 可誘導鐵死亡、凋亡和自噬。
Sulfasalazine Chemical Structure
CAS: 599-79-1
產(chǎn)品質(zhì)控
批次：
純度：
99.86%
99.86
Sulfasalazine相關產(chǎn)品
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息(PMID) |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Sulfasalazine是一種磺胺劑，是Mesalazine的衍生物，主要用作抗炎劑。Sulfasalazine 是一種有效的、特異性的 nuclear factor kappa B (NF-κB)、TGF-β 和 COX-2 的抑制劑。Sulfasalazine 可誘導鐵死亡、凋亡和自噬。 | |||
|---|---|---|---|---|
| 靶點 |
|
| 體外研究(In Vitro) | ||||
| 體外研究活性 | Sulfasalazin，像甲氨蝶呤一樣，增強了發(fā)炎部位釋放腺苷，并且腺苷通過炎癥細胞的A2受體減少炎癥。[1] Sulfasalazin處理4小時抑制κB依賴性轉(zhuǎn)錄，IC 50值大約為0.625 mM。Sulfasalazin（2.5 mM）以劑量和時間依賴性導致T淋巴細胞的細胞死亡。Sulfasalazin，但不是5ASA或者sulfapyridine，強力抑制NF-κB活化并有力地誘導T淋巴細胞的細胞凋亡。[2] Sulfasalazin通過結(jié)腸細菌裂解成sulfapyridine和5-氨基水楊酸（5-ASA;mesalamine），而后者也抑制NF-κB活性。Sulfasalazin但不是其裂解形式5-ASA劑量依賴性抑制膠質(zhì)瘤的增長，這種效果是完全歸因于胱氨酸攝取，經(jīng)由系統(tǒng)x(c)中抑制(- )胱氨酸谷氨酸轉(zhuǎn)運。Sulfasalazin抑制胱氨酸攝入,引起細胞內(nèi)谷胱甘肽的慢性消耗，從而破壞細胞的氧化還原防御,阻礙腫瘤生長。[3] |
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|---|---|---|---|---|
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 在小鼠氣囊模型中，Sulfasalazin顯著降低發(fā)炎(carrageenan, 2 毫克/毫升)氣囊中積累的白細胞的數(shù)量。Sulfasalazin處理促進splenocyte 5-aminoimidazole-4-carboxamidoribonucleotide (AICAR)濃度的顯著增加，和體外觀察到的Sulfasalazin抑制AICAR甲酰基轉(zhuǎn)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 |
|
化學信息&溶解度
| 分子量 | 398.39 | 分子式 | C18H14N4O5S |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 80 mg/mL ( (200.8 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
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體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | |||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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