Balcinrenone
Based on 1 Customer Validation
Balcinrenone (AZD9977) is a potent, selective, and orally active mineralocorticoid receptor (MR) modulator. Balcinrenone is used for heart failure, and chronic kidney disease research.
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: 99.62%
- CAS 番号: 1850385-64-6
- 分子式: C20H18FN3O5
- 分子量:399.37
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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
Balcinrenone (AZD9977) and eplerenone activities on MR, GR, PR and AR in binding assays. The observed pKi of MR, GR, and PR are 7.5, 5.4 and 4.6, respectively.Functional interaction of Balcinrenone with MR is characterized in a reporter gene assay where the full-length MR drives a luciferase reporter gene in U2-OS cells. Balcinrenone antagonizes aldosterone-activated MR with an IC50 of 0.28 μM. Whereas eplerenone is a full antagonist, Balcinrenone suppresses only 69% of the MR activity in this assay. Species selective potencies of Balcinrenone are established in reporter gene assays using the MR LBDs from human, mouse or rat. The corresponding IC50 values are 0.37 μM, 0.08 μM and 0.08μM, respectively.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Uni-nephrectomised male Sprague Dawley rats administered aldosterone and fed a high-salt diet with AZD9977[1]
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Dosage:10, 30 and 100 mg/kg
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Administration:Oral administration; 10-100 mg/kg; 4 weeks
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Result:Improved kidney function and histology in animal models of CKD.
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Animal Model:Db/db mice uni-nephrectomised at 8 weeks of age are treated from age 18w to age 22w[1]
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Dosage:100 mg/kg
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Administration:Oral administration; 100 mg/kg; co-administration with enalapril
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Result:Reduced albuminuria in diabetic kidney disease.Co-administration of enalapril with AZD9977 had an additive effect on renal pathology scoring.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1850385-64-6
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性状 Solid
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分子量 399.37
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分子式 C20H18FN3O5
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Color White to off-white
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SMILES
FC1=CC2=C(N(C(C3=CC=C(OCC(N4)=O)C4=C3)=O)[C@@H](CC(NC)=O)CO2)C=C1
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別名
AZD9977
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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 : 250 mg/mL (625.99 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: ≥ 2.08 mg/mL (5.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.21 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 (279 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 | 2.5039 mL | 12.5197 mL | 25.0394 mL | 62.5986 mL |
| 5 mM | 0.5008 mL | 2.5039 mL | 5.0079 mL | 12.5197 mL | |
| 10 mM | 0.2504 mL | 1.2520 mL | 2.5039 mL | 6.2599 mL | |
| 15 mM | 0.1669 mL | 0.8346 mL | 1.6693 mL | 4.1732 mL | |
| 20 mM | 0.1252 mL | 0.6260 mL | 1.2520 mL | 3.1299 mL | |
| 25 mM | 0.1002 mL | 0.5008 mL | 1.0016 mL | 2.5039 mL | |
| 30 mM | 0.0835 mL | 0.4173 mL | 0.8346 mL | 2.0866 mL | |
| 40 mM | 0.0626 mL | 0.3130 mL | 0.6260 mL | 1.5650 mL | |
| 50 mM | 0.0501 mL | 0.2504 mL | 0.5008 mL | 1.2520 mL | |
| 60 mM | 0.0417 mL | 0.2087 mL | 0.4173 mL | 1.0433 mL | |
| 80 mM | 0.0313 mL | 0.1565 mL | 0.3130 mL | 0.7825 mL | |
| 100 mM | 0.0250 mL | 0.1252 mL | 0.2504 mL | 0.6260 mL |
Balcinrenone 関連分類
HY-120274 関連分類
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