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Sulindac
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Sulindac图片
CAS NO:38194-50-2
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
500mg电议
1 g电议
5 g电议

产品名称
舒林酸
MK-231
产品介绍
Sulindac (MK-231) 是一种口服活性非甾体类抗炎药。Sulindac 也是一种免疫调节剂。Sulindac 可用于脊柱关节炎、痛风性关节炎及多种癌症如结直肠癌、肺癌的研究。
生物活性

Sulindac (MK-231) is an orally active nonsteroidalanti-inflammatoryagent. Sulindac also is an immunomodulatory agent. Sulindac can be used for the research of arthritis of the spine, gouty arthritis and kinds ofcancerincluding colorectalcancer(CRC) and lungcancer[1][2].

IC50& Target[1]

COX-2

 

Autophagy

 

体外研究
(In Vitro)

Sulindac (MK-231) (500 μM, 48 h) is effective in preventing TGF-β1-induced EMT, as indicated by upregulation of the epithelial marker, E-cadherin, and downregulation of mesenchymal markers and transcription factors[1].
Sulindac (500 μM, 48 h) can inhibit TGF-β1-enhanced migration and invasion of A549 cells[1].
Sulindac (500 μM, 48 h) enhances the reversal of TGF-β1-induced EMT by sulindac and SIRT1 upregulation promoted TGF-β1-induced EMT[1].

Western Blot Analysis[1]

Cell Line:A549 cells
Concentration:500 μM
Incubation Time:48 h
Result:Inhibit transforming growth factor (TGF)-β1-induced epithelial-mesenchymal transition in A549 cells.

Immunofluorescence[1]

Cell Line:A549 cells
Concentration:500 μM
Incubation Time:48 h
Result:Reversed SIRT-1 expression by TGF-β1 and inhibited the TGF-β1-induced cadherin switch.

Cell Migration Assay[1]

Cell Line:A549 cells
Concentration:500 μM
Incubation Time:48 h
Result:Inhibited migration, decreased resistance co-treatment with TGF-β1.

Cell Invasion Assay[1]

Cell Line:A549 cells
Concentration:500 μM
Incubation Time:40 h; 48 h
Result:Could effectively inhibit the TGF- β1-induced increase in invasion by lung cancer cells.
体内研究
(In Vivo)

Sulindac (MK-231) (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) shows a significant reduction in tumor volume and increases infiltration of CD8+ T lymphocytes in the tumor tissues when treated with combination therapy[2].
Sulindac (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) can downregulate PD-L1 by blocking NF-κB signaling, which in turn led to a decrease in exosomal P[2].
Sulindac (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) leads to increased availability of PD-L1 Ab by downregulating PD-L1 in combination therapy[2].
Sulindac (15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)) has not a systemic inhibitory effect on prostaglandin E2 (PGE2) in low-dose does[2].

Animal Model:CT26 syngeneic mouse tumor model[2]
Dosage:15 mg/kg; 7.5 mg/kg
Administration:15 mg/kg, p.o., bid (sulindac alone); 7.5 mg/kg p.o., bid (sulindac combination with PD-L1)
Result:Downregulated PD-L1 through the blockade of NF-κB signaling and modulate the response of pMMR CRC to anti-PD-L1 immunotherapy.
Cound effectively inhibit PD-L1 with no significant systematic toxicity.
Clinical Trial
分子量

356.41

性状

Solid

Formula

C20H17FO3S

CAS 号

38194-50-2

中文名称

舒林酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL(140.29 mM;Need ultrasonic)

H2O :< 0.1 mg/mL(insoluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8058 mL14.0288 mL28.0576 mL
5 mM0.5612 mL2.8058 mL5.6115 mL
10 mM0.2806 mL1.4029 mL2.8058 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (7.01 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.01 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.5 mg/mL (7.01 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.01 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在本网站选购。