Sulindac sulfide (Synonyms: cis-Sulindac sulfide) |
Catalog No.GC15059
One-Click Copy Product Info
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Sulindac sulfide는 γ42-secretase 활성에 대한 IC50이 20.2μM인 비경쟁적 γ-secretase 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 49627-27-2
Sample solution is provided at 25 µL, 10mM.
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Sulindac is a non-steroidal anti-inflammatory drug that has an extensive epidemiology documenting reduced human colorectal cancer. In mouse models, sulindac was found not only to inhibit the enzymatic activity of polyp-associated COX-2, but also to downregulate the expression of colonic COX-2 protein to control levels.[1] Sulindac sulfide is a metabolite of sulindac that has diverse activities.[2],[3] It inhibits both COX-1 and COX-2 (IC50s = 1.9 and 1.21 µM, respectively), whereas the parent compound, sulindac, is much less effective (IC50 = 58 µM for COX-2 and > 100 µM for COX-1).[4] Sulindac sulfide also inhibits aldose reductase (IC50 = 279 nM), blocking NADPH-dependent reduction of glucose to sorbitol, and reducing type 2 diabetic complications.[5] It increases the expression and activity of NAD(P)H quinone oxidoreductase [1].[6] Sulindac sulfide inhibits colorectal cancer growth both in vitro and in vivo.[7]
Reference:
[1]. Boolbol, S.K., Dannenberg, A.J., Chadburn, A., et al. Cyclooxygenase-2 overexpression and tumor formation are blocked by sulindac in a murine model of familial adenomatous polyposis. Cancer Research 56, 2556-2560 (1996).
[2]. Kitamura, S., and Tatsumi, K. In vitro metabolism of sulindac and sulindac sulfide: Enzymatic formation of sulfoxide and sulfone. Japanese Journal of Pharmacology 32(5), 833-838 (1982).
[3]. Brunell, D., Sagher, D., Kesaraju, S., et al. Studies on the metabolism and biological activity of the epimers of sulindac. Drug Metabolism and Disposition 39(6), 1014-1021 (2011).
[4]. Warner, T.D., Giuliano, F., Vojnovic, I., et al. Nonsteroid drug selectivities for cyclo-oxygenase-1 rather than cyclo-oxygenase-2 are associated with human gastrointestinal toxicity: A full in vitro analysis. Proc. Nat. Acad. Sci. USA 96(13), 7563-7568 (1999).
[5]. Zheng, X., Zhang, L., Zhai, J., et al. The molecular basis for inhibition of sulindac and its metabolites towards human aldose reductase. FEBS Letters 586(1), 55-59 (2012).
[6]. Kung, H.N., Weng, T.Y., Liu, Y.L., et al. Sulindac compounds facilitate the cytotoxicity of β-lapachone by up-regulation of NAD(P)H quinone oxidoreductase in human lung cancer cells. PLoS One 9(2), 1-15 (2014).
[7]. Williams, C.S., Goldman, A.P., Sheng, H., et al. Sulindac sulfide, but not sulindac sulfone, inhibits colorectal cancer growth. Neoplasia 1(2), 170-176 (1999).
| Cas No. | 49627-27-2 | SDF | |
| Synonyms | cis-Sulindac sulfide | ||
| Chemical Name | (Z)-2-(5-fluoro-2-methyl-1-(4-(methylthio)benzylidene)-1H-inden-3-yl)acetic acid | ||
| Canonical SMILES | FC1=CC2=C(/C(C(C)=C2CC(O)=O)=C\C3=CC=C(SC)C=C3)C=C1 | ||
| Formula | C20H17FO2S | M.Wt | 340.41 |
| Solubility | 2mg/mL in ethanol, 30mg/mL in DMSO, or in DMF | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9376 mL | 14.6882 mL | 29.3763 mL |
| 5 mM | 587.5 μL | 2.9376 mL | 5.8753 mL |
| 10 mM | 293.8 μL | 1.4688 mL | 2.9376 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)