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抑制剂/激动剂
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环氧合酶抑制剂
环氧化酶 环氧合酶
/ Sulindac

舒林酸 /Sulindac {[allProObj[0].p_purity_real_show]}

货号：A253022 同义名： MK-231

Sulindac是一种非类固醇抗炎药（NSAID），被认为作用于COX-1和COX-2酶，抑制前列腺素合成。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Sulindac 化学结构 CAS号：38194-50-2
Sulindac 化学结构
CAS号：38194-50-2
Sulindac 3D分子结构
CAS号：38194-50-2
Sulindac 化学结构 CAS号：38194-50-2
Sulindac 3D分子结构 CAS号：38194-50-2
规格 价格 会员价 库存 数量
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Sulindac 纯度/质量文件 产品仅供科研

货号：A253022 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 COX ↓ COX-1 ↓ COX-2 ↓ 其他靶点 纯度
Piroxicam ✔ 98%
Salicylic acid ✔ 98%
Phenacetin ✔ 98%
Etodolac ✔ 99%
Flunixin meglumine ✔ 98%
Ibuprofen L-lysine ✔ 99%
Nabumetone ✔ 98%
Acemetacin ✔ 98%
Diflunisal ✔ 98%
Pranoprofen ✔ 98%
Ampiroxicam ✔ 98%
Meloxicam ✔ 98%
Sulindac ✔ 98%
Ketoprofen ✔ 98%
Mefenamic Acid ✔ 95%
Bromfenac sodium ✔ 98%
Oxaprozin ✔ 99%
Aspirin ✔ 99%
Nepafenac ✔ 98%
Zaltoprofen ✔ 99%
Salicin ✔ 98%
Suprofen ✔ 99%+
Xanthohumol ✔ 99%
Parecoxib ✔ 98%
Tolfenamic Acid +++

COX-2, IC50: 0.2 μM

 		98%
Etoricoxib ✔ 99%
Niflumic Acid ✔ 98%
Valdecoxib ++++

COX-2, IC50: 5 nM

 		99+%
Ibuprofen +

COX-1, IC50: 13 μM

 		+

COX-2, IC50: 370 μM

 		98%
Indomethacin ++

COX1, IC50: 0.28 μM

 		+

COX-2, IC50: 14 μM

 		97%
Lornoxicam ++++

COX-1, IC50: 5 nM

 		++++

COX-2, IC50: 8 nM

 		98%
Meclofenamic acid sodium ++++

COX-1, IC50: 40 nM

 		+++

COX-2, IC50: 50 nM

 		99%
Rofecoxib ++++

COX-2, IC50: 18 nM

 		98%
Asaraldehyde ✔ 98%
Naproxen +

COX-1, IC50: 8.7 μM

 		+

COX-2, IC50: 5.2 μM

 		98%
Diclofenac Sodium Salt +++

COX-1, IC50: 60 nM

 		+++

COX-2, IC50: 200 nM

 		98%
NS-398 ++

COX-2, IC50: 3.8 μM

 		95%
Amfenac Sodium Hydrate ++

COX-1, IC50: 250 nM

 		+++

COX-2, IC50: 150 nM

 		98%+
Nimesulide +

COX-2, IC50: 26 μM

 		98%
Lumiracoxib ++

COX-1, Ki: 3 μM

 		+++

COX-2, Ki: 60 nM

 		99%
Rutaecarpine ✔ 95%
Celecoxib ++++

COX-2, IC50: 40 nM

 		98%
Carprofen ++++

canine COX2, IC50: 30 nM

 		98%
Ketorolac ++

COX-1 (human), IC50: 1.23 μM

 		++

COX-2 (human), IC50: 3.50 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Sulindac 生物活性

靶点

  • COX
描述 Sulindac is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2. Treatment with sulindac not only inhibited tumor formation but decreased small bowel Cox-2 and prostaglandin E(2) to baseline and restored normal levels of apoptosis[3]. Sulindac (0.1 mM to 0.5 mM) causes limited death in both p53 wt and p53 null HCT116 cells, but in combination with vitamin C, it dramatically increases almost 5-fold in cell death in p53 wt HCT116 cells relative to the vitamin C alone, and such an effect is involving caspase activation and p53 function in these cells, and via ROS-mediated pathway. Sulindac combined with vitamin C significantly increases PUMA levels, but shows no effect on Bim, Bcl-2 and Mcl-1 levels[4]. Moreover, celecoxib and sulindac can inhibit TGF-β1-induced EMT (epithelial-mesenchymal transition) and suppress lung cancer cell migration and invasion via downregulation of SIRT1(class III deacetylase sirtuin 1) [5]. Sulindac can protect normal astrocytes against oxidative stress. Sulindac induces differentiation of both NSC ( neural stem cells) and GSC (glioblastoma stem cells) cells and sulindac upregulates neurogenesis in NSC. The differentiated NSC are also protected from oxidative stress damage, whereas the differentiation of GSC by sulindac increases the sensitivity of these cells to agents that cause oxidative stress[6].

Sulindac 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00275756 Glaucoma Not Applicable Withdrawn - Austria ... 展开 >> Department of Clinical Pharmacology Vienna, Austria, A-1090 收起 <<
NCT00283803 - Completed - -
NCT02003703 Hepatitis B H... 展开 >>IV 收起 << Phase 3 Recruiting - Chile ... 展开 >> Hospital Gustavo Fricke Recruiting Viña del Mar, Valparaíso, Chile Contact: Jose I Vargas, MD    62473415 ext +56 9    jivargasd@icloud.com    Contact: Daniela Jensen, MD    62473409 ext +56 9    daniela_jensen@hotmail.com    Principal Investigator: Jose I Vargas, MD          Principal Investigator: Daniela Jensen, MD          Principal Investigator: Francisco Fuster, MD          Principal Investigator: Valeska Sarmiento 收起 <<

Sulindac 参考文献

[1]Yamamoto Y, Yin MJ, et al. Sulindac inhibits activation of the NF-kappaB pathway. J Biol Chem. 1999 Sep 17;274(38):27307-14.

[2]Piazza GA, Rahm AL, et al. Antineoplastic drugs sulindac sulfide and sulfone inhibit cell growth by inducing apoptosis. Cancer Res. 1995 Jul 15;55(14):3110-6.

[3]Boolbol SK, Dannenberg AJ, Chadburn A, et al. Cyclooxygenase-2 overexpression and tumor formation are blocked by sulindac in a murine model of familial adenomatous polyposis. Cancer Res. 1996;56(11):2556-2560

[4]Gong EY, Shin YJ, Hwang IY, et al. Combined treatment with vitamin C and sulindac synergistically induces p53- and ROS-dependent apoptosis in human colon cancer cells. Toxicol Lett. 2016;258:126-133

[5]Cha BK, Kim YS, Hwang KE, et al. Celecoxib and sulindac inhibit TGF-β1-induced epithelial-mesenchymal transition and suppress lung cancer migration and invasion via downregulation of sirtuin 1. Oncotarget. 2016;7(35):57213-5722

[6]Allani SK, Weissbach H, Lopez Toledano MA. Sulindac induces differentiation of glioblastoma stem cells making them more sensitive to oxidative stress. Neoplasma. 2018;65(3):376-388

Sulindac 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.81mL

0.56mL

0.28mL

14.03mL

2.81mL

1.40mL

28.06mL

5.61mL

2.81mL

Sulindac 技术信息

CAS号38194-50-2
分子式C20H17FO3S
分子量 356.411
别名 MK-231
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,Store in freezer, under -20°C
溶解方案

DMSO: 50 mg/mL(140.29 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二
动物实验配方

Tags: Sulindac | 38194-50-2 | MK-231 | MK231 | MK 231 | NF-κB | Immunology/Inflammation | NF-κB | PD-1/PD-L1 | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Sulindac 纯度/质量文件 | Sulindac 亚型比较 | Sulindac 生物活性 | Sulindac 临床数据 | Sulindac 参考文献 | Sulindac 实验方案 | Sulindac 技术信息

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