Fuzapladib
Based on 1 Customer Validation
Fuzapladib (IS-741), an orally active leukocyte-function-associated antigen type 1 (LFA-1) activation inhibitor, is a leukocyte adhesion molecule. Fuzapladib is also a phospholipase A2 (PLA2) inhibitor. Fuzapladib exerts anti-inflammatory effects by inhibiting leukocyte migration into the inflammatory site.
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 : 98.75%
- CAS 番号: 141283-87-6
- 分子式: C15H20F3N3O3S
- 分子量:379.40
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Phospholipase アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
体外実験
Fuzapladib (IS-741) (1 μM, 3 h) can significantly inhibit the adhesion of HL-60 cells to HUVEC under the stimulation of lipopolysaccharide[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[4]
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Dosage:50 mg/kg
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Administration:P.o.; for 7 days
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Result:Significantly reduced myeloperoxidase (MPO) activity and mucosal IL-8 levels in rat ileum, reduced polymorphonuclear cells and Mac-1 positivity Infiltration of cells into inflammatory lesions, effectively alleviated trinitrobenzenesulfonic acid (TNBS)-induced ileitis.
化学情報
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CAS 番号 141283-87-6
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性状 Solid
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分子量 379.40
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分子式 C15H20F3N3O3S
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Color White to off-white
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SMILES
O=C(C1CCCCC1)NC2=CC(C(F)(F)F)=CN=C2NS(=O)(CC)=O
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別名
IS-741
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (263.57 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 (protect from light). 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 (protect from light). 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)
体内:
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.59 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
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- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Noriyuki Kaji, et al. Fuzapladib reduces postsurgical inflammation in the intestinal muscularis externa. J Vet Med Sci. 2023 Sep 21. [Content Brief]
[2]. C Bassi. IS-741 (Ishihara Sangyo). Curr Opin Investig Drugs. 2001 Apr;2(4):510-2. [Content Brief]
[3]. Shikama H, et al. Effect of IS-741 on cell adhesion between human umbilical vein endothelial cells and HL-60 cells. Biol Pharm Bull. 1999 Feb;22(2):127-31. [Content Brief]
[4]. Tetsuya Fukunaga, et al. A novel diamino-pyridine derivative (IS-741) attenuates rat ileitis induced by trinitrobenzene sulfonic acid. J Gastroenterol. 2003;38(5):451-9. [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 (protect from light). 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 | 2.6357 mL | 13.1787 mL | 26.3574 mL | 65.8935 mL |
| 5 mM | 0.5271 mL | 2.6357 mL | 5.2715 mL | 13.1787 mL | |
| 10 mM | 0.2636 mL | 1.3179 mL | 2.6357 mL | 6.5894 mL | |
| 15 mM | 0.1757 mL | 0.8786 mL | 1.7572 mL | 4.3929 mL | |
| 20 mM | 0.1318 mL | 0.6589 mL | 1.3179 mL | 3.2947 mL | |
| 25 mM | 0.1054 mL | 0.5271 mL | 1.0543 mL | 2.6357 mL | |
| 30 mM | 0.0879 mL | 0.4393 mL | 0.8786 mL | 2.1965 mL | |
| 40 mM | 0.0659 mL | 0.3295 mL | 0.6589 mL | 1.6473 mL | |
| 50 mM | 0.0527 mL | 0.2636 mL | 0.5271 mL | 1.3179 mL | |
| 60 mM | 0.0439 mL | 0.2196 mL | 0.4393 mL | 1.0982 mL | |
| 80 mM | 0.0329 mL | 0.1647 mL | 0.3295 mL | 0.8237 mL | |
| 100 mM | 0.0264 mL | 0.1318 mL | 0.2636 mL | 0.6589 mL |
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