Derenofylline
Based on 3 publication(s) in Google Scholar
Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats.
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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: 99.93%
- CAS 番号: 251945-92-3
- 分子式: C18H20N4O
- 分子量:308.38
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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MedChemExpress（MCE）の使用を引用している文献 Derenofylline
MoreAdenosine Receptor 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
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A1R 1 nM (Ki) |
Adenosine A3 receptor 200 nM (Ki) |
A2AR 398 nM (Ki) |
Derenofylline (100 μM, 72 h) inhibits TGF-β1-induced myofibroblast transformation without affecting the cell viability[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Derenofylline (10 mg/kg/d, oral administration, 12 weeks) reduces myocardial fibrosis in 5/6 nephrectomy rats without affecting blood pressure[1].
Derenofylline (0.1-5mg/kg, intravenous injection) causes no major haemodynamic effects (heart rate and blood pressure)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5/6 nephrectomy rats[1]
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Dosage:10 mg/kg/d
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Administration:Oral administration, mixed with food for 12 weeks
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Result:Attenuated urinary albuminuria by about 50%.
Suppressed the increase in CK levels, ALT and AST plasma levels in nephrectomized animals.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 251945-92-3
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性状 Solid
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分子量 308.38
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分子式 C18H20N4O
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Color White to off-white
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SMILES
O[C@H]1CC[C@H](NC2=C3C(NC=C3)=NC(C4=CC=CC=C4)=N2)CC1
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別名
SLV 320
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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 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Antioxidants (Basel)
A Novel SIRT1 Activator Hydroxygenkwanin Alleviates Osteoporosis by Inhibiting Ferroptosis and Lactylation in Skeletal Stem/Progenitor Cells. [Abstract]2026 May 12;15(5):612. PMID: 42193234 -
溶剤 & 溶解度
DMSO : 100 mg/mL (324.28 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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: ≥ 6.25 mg/mL (20.27 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (20.27 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
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- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kalk P, et al. The adenosine A1 receptor antagonist SLV320 reduces myocardial fibrosis in rats with 5/6 nephrectomy without affecting blood pressure. Br J Pharmacol. 2007 Aug;151(7):1025-32. [Content Brief]
[2]. Marta Mateus, et al. Understanding the Role of Adenosine Receptors in the Myofibroblast Transformation in Peyronie's Disease. J Sex Med. 2018 Jul;15(7):947-957. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2428 mL | 16.2138 mL | 32.4275 mL | 81.0688 mL |
| 5 mM | 0.6486 mL | 3.2428 mL | 6.4855 mL | 16.2138 mL | |
| 10 mM | 0.3243 mL | 1.6214 mL | 3.2428 mL | 8.1069 mL | |
| 15 mM | 0.2162 mL | 1.0809 mL | 2.1618 mL | 5.4046 mL | |
| 20 mM | 0.1621 mL | 0.8107 mL | 1.6214 mL | 4.0534 mL | |
| 25 mM | 0.1297 mL | 0.6486 mL | 1.2971 mL | 3.2428 mL | |
| 30 mM | 0.1081 mL | 0.5405 mL | 1.0809 mL | 2.7023 mL | |
| 40 mM | 0.0811 mL | 0.4053 mL | 0.8107 mL | 2.0267 mL | |
| 50 mM | 0.0649 mL | 0.3243 mL | 0.6486 mL | 1.6214 mL | |
| 60 mM | 0.0540 mL | 0.2702 mL | 0.5405 mL | 1.3511 mL | |
| 80 mM | 0.0405 mL | 0.2027 mL | 0.4053 mL | 1.0134 mL | |
| 100 mM | 0.0324 mL | 0.1621 mL | 0.3243 mL | 0.8107 mL |
Derenofylline 関連分類
HY-14858 関連分類
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