Zelasudil
Based on 1 Customer Validation
Zelasudil (RXC007) is an orally active, highly selective small molecule Rho-associated coiled-coil containing protein kinase 2 (ROCK2) inhibitor with anti-fibrotic efficacy. Zelasudil elicits positive immunomodulatory effects in metastatic pancreatic tumors with increase of CD8+ and CD4+ T cell infiltrate into the tumor cortex and reduction in immunosuppressive FOXP3+ regulatory T cells at the tumor border. Zelasudil is promising for research of pancreatic ductal adenocarcinoma.
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: 99.48%
- CAS 番号: 2365193-22-0
- 分子式: C22H21F2N7O
- 分子量:437.45
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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
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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Bleomycin (HY-108345)-induced lung fibrosis mouse model[4]
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Dosage:5-100 mg/kg
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Administration:p.o., a single dose for 21 days
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Result:Significantly reduced fibrosis and collagen deposition and picrosirius red in the lung.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2365193-22-0
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性状 Solid
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分子量 437.45
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分子式 C22H21F2N7O
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Color Off-white to light brown
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SMILES
O=C(C1=CC=C(C2=NN(C)C(NC3=CC=C4NN=CC4=C3C5CC5)=N2)C=C1)NCC(F)F
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別名
RXC007
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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
溶剤 & 溶解度
DMSO : 100 mg/mL (228.60 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: 2.5 mg/mL (5.71 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (5.71 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
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 (273 KB)
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SDS (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 2.2860 mL | 11.4299 mL | 22.8598 mL | 57.1494 mL |
| 5 mM | 0.4572 mL | 2.2860 mL | 4.5720 mL | 11.4299 mL | |
| 10 mM | 0.2286 mL | 1.1430 mL | 2.2860 mL | 5.7149 mL | |
| 15 mM | 0.1524 mL | 0.7620 mL | 1.5240 mL | 3.8100 mL | |
| 20 mM | 0.1143 mL | 0.5715 mL | 1.1430 mL | 2.8575 mL | |
| 25 mM | 0.0914 mL | 0.4572 mL | 0.9144 mL | 2.2860 mL | |
| 30 mM | 0.0762 mL | 0.3810 mL | 0.7620 mL | 1.9050 mL | |
| 40 mM | 0.0571 mL | 0.2857 mL | 0.5715 mL | 1.4287 mL | |
| 50 mM | 0.0457 mL | 0.2286 mL | 0.4572 mL | 1.1430 mL | |
| 60 mM | 0.0381 mL | 0.1905 mL | 0.3810 mL | 0.9525 mL | |
| 80 mM | 0.0286 mL | 0.1429 mL | 0.2857 mL | 0.7144 mL | |
| 100 mM | 0.0229 mL | 0.1143 mL | 0.2286 mL | 0.5715 mL |
Zelasudil 関連分類
HY-148808 関連分類
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