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Synonyms | FIN, BAY 94-8862 | Storage (From the date of receipt) |
3 years -20°C powder | ||||
化学式 | C21H22N4O3 |
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分子量 | 378.42 | CAS No. | 1050477-31-0 | ||||
Solubility (25°C)* | 体外 | DMSO | 76 mg/mL (200.83 mM) | ||||
Ethanol | 10 mg/mL (26.42 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Finerenone (FIN, BAY 94-8862) is a highly selective and orally available nonsteroidal antagonist of mineralocorticoid receptor (MR) with IC50 of 18 nM. Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease. |
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in vitro | In vitro, Finerenone dose-dependently reduces aldosterone-induced smooth muscle cell (SMC) proliferation and prevents aldosteroneinduced endothelial cell (EC) apoptosis. Finerenone significantly reduces apoptosis of ECs and simultaneously attenuates SMC proliferation, resulting in accelerated endothelial healing and reduced neointima formation of the injured vessels.[2] |
in vivo | Finerenone improves endothelial dysfunction through an enhancement in NO bioavailability and a decrease in superoxide anion levels due to an upregulation in SOD activity. This is associated with an increase in renal SOD activity and a reduction of albuminuria.[1] |
細胞アッセイ | 細胞株 | Human coronary artery smooth muscle cells (SMC), human umbilical vein endothelial cells (EC) |
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濃度 | 1 nM, 10 nM | |
反応時間 | 24 h | |
実験の流れ | Cells are incubated with aldosterone with or without finerenone for 24 hours after 24 hours of serum-starvation for the assessment of cell proliferation and apoptosis. Immediately prior to the addition of aldosterone, cells are preincubated with finerenone or vehicle for 30 minutes. |
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動物実験 | 動物モデル | 12-week-old MWF, aged-matched normoalbuminuric Wistar rats |
投薬量 | 10 mg/kg | |
投与方法 | Oral gavage |
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長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。