Exisulind
Based on 2 publication(s) in Google Scholar
Exisulind is an inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac. Exisulind inhibits aldose reductase with an IC50 of 367 nM in vitro and may contribute to the beneficial pharmacological effects of sulindac on type 2 diabetic complications.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.04%
- CAS 番号: 59864-04-9
- 分子式: C20H17FO4S
- 分子量:372.41
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 Exisulind
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COLO 320 | IC50 |
>200 μM
Compound: b
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Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay
Cytotoxicity against human COLO320 cells after 72 hrs by WST-1 assay
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[PMID: 20801552] |
| MIA PaCa-2 | IC50 |
>200 μM
Compound: b
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Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay
Cytotoxicity against human MIAPaCa2 cells after 72 hrs by WST-1 assay
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[PMID: 20801552] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 59864-04-9
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性状 Solid
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分子量 372.41
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分子式 C20H17FO4S
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Color Light yellow to yellow
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SMILES
O=C(O)CC(C1=C/2C=CC(F)=C1)=C(C)C2=C/C3=CC=C(S(=O)(C)=O)C=C3
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別名
スリンダクスルホン
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Pharmacol Res
Identification of Fasudil as a collaborator to promote the anti-tumor effect of lenvatinib in hepatocellular carcinoma by inhibiting GLI2-mediated hedgehog signaling pathway. [Abstract]2024 Feb:200:107082. PMID: 38280440 -
Life Sci
2024 Jun 1:346:122631. PMID: 38621585
溶剤 & 溶解度
DMSO : 100 mg/mL (268.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1 mg/mL (2.69 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1 mg/mL (2.69 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kitamura S, Tatsumi K. In vitro metabolism of sulindac and sulindac sulfide: enzymatic formation of sulfoxide and sulfone. Jpn J Pharmacol. 1982 Oct;32(5):833-8. [Content Brief]
[2]. Zheng X, et al. The molecular basis for inhibition of sulindac and its metabolites towards human aldose reductase. FEBS Lett. 2012 Jan 2;586(1):55-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6852 mL | 13.4261 mL | 26.8521 mL | 67.1303 mL |
| 5 mM | 0.5370 mL | 2.6852 mL | 5.3704 mL | 13.4261 mL | |
| 10 mM | 0.2685 mL | 1.3426 mL | 2.6852 mL | 6.7130 mL | |
| 15 mM | 0.1790 mL | 0.8951 mL | 1.7901 mL | 4.4754 mL | |
| 20 mM | 0.1343 mL | 0.6713 mL | 1.3426 mL | 3.3565 mL | |
| 25 mM | 0.1074 mL | 0.5370 mL | 1.0741 mL | 2.6852 mL | |
| 30 mM | 0.0895 mL | 0.4475 mL | 0.8951 mL | 2.2377 mL | |
| 40 mM | 0.0671 mL | 0.3357 mL | 0.6713 mL | 1.6783 mL | |
| 50 mM | 0.0537 mL | 0.2685 mL | 0.5370 mL | 1.3426 mL | |
| 60 mM | 0.0448 mL | 0.2238 mL | 0.4475 mL | 1.1188 mL | |
| 80 mM | 0.0336 mL | 0.1678 mL | 0.3357 mL | 0.8391 mL | |
| 100 mM | 0.0269 mL | 0.1343 mL | 0.2685 mL | 0.6713 mL |