Eplerenone

製品コードS1707 バッチS170703

化学情報

	Synonyms	CGP 30083, SC-66110	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₄H₃₀O₆
	分子量	414.49	CAS No.	107724-20-9
Solubility (25°C)*	体外	DMSO	11 mg/mL warmed with 50ºC water bath (26.53 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Eplerenone is a mineralocorticoid receptor antagonist, and blocks the action of aldosterone, used to control high blood pressure.
in vivo	Eplerenone inhibits upregulated phosphorylation of PKCepsilon, MAP kinase, and p90RSK in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone increases downregulated endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone administration results in significant improvement in glomerulosclerosis and urinary protein in DS rats. ^[1] Eplerenone (200 mg/kg/day) administration significantly decreases systolic and diastolic blood pressure by 12% and 11%, respectively, compared with untreated mice. Eplerenone increases serum susceptibility to lipid peroxidation decreased by as much as 26%, and serum paraoxonase activity in mice. Eplerenone significantly reduces the atherosclerotic lesion area in aortas of mice, and this effect is reversed by AT-II. ^[2] Eplerenone increases total vessel area by 30% and luminal area by nearly 60% compared with the no-treatment group, without affecting neointima size in pigs. ^[3] Eplerenone significantly decreases LV end-diastolic wall stress in dogs. Eplerenone is associated with a 28% reduction in cardiomyocyte cross-sectional area, a 37% reduction of volume fraction of reactive interstitial fibrosis, and a 34% reduction of volume fraction of replacement fibrosis in dogs with heart failure. ^[4] Eplerenone blunts the increase in pulse pressure in Aldo rats and normalized Einc-wall stress curves, medial cross-sectional area (MCSA), and EIIIA fibronectin in aldosterone (Aldo)-salt hypertensive rats. ^[5]

製品説明

Eplerenone is a mineralocorticoid receptor antagonist, and blocks the action of aldosterone, used to control high blood pressure.

in vivo

Eplerenone inhibits upregulated phosphorylation of PKCepsilon, MAP kinase, and p90RSK in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone increases downregulated endothelial nitric oxide synthase mRNA in Dahl salt-sensitive hypertensive (DS) rats. Eplerenone administration results in significant improvement in glomerulosclerosis and urinary protein in DS rats. ^[1] Eplerenone (200 mg/kg/day) administration significantly decreases systolic and diastolic blood pressure by 12% and 11%, respectively, compared with untreated mice. Eplerenone increases serum susceptibility to lipid peroxidation decreased by as much as 26%, and serum paraoxonase activity in mice. Eplerenone significantly reduces the atherosclerotic lesion area in aortas of mice, and this effect is reversed by AT-II. ^[2] Eplerenone increases total vessel area by 30% and luminal area by nearly 60% compared with the no-treatment group, without affecting neointima size in pigs. ^[3] Eplerenone significantly decreases LV end-diastolic wall stress in dogs. Eplerenone is associated with a 28% reduction in cardiomyocyte cross-sectional area, a 37% reduction of volume fraction of reactive interstitial fibrosis, and a 34% reduction of volume fraction of replacement fibrosis in dogs with heart failure. ^[4] Eplerenone blunts the increase in pulse pressure in Aldo rats and normalized Einc-wall stress curves, medial cross-sectional area (MCSA), and EIIIA fibronectin in aldosterone (Aldo)-salt hypertensive rats. ^[5]

プロトコル(参考用のみ)

参考

+ 展开

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Chronic stress promotes glioma cell proliferation via the PI3K/Akt signaling pathway [ Oncol Rep, 2021, 46(3)202]	PubMed: 34296295
[ BMJ Open Diabetes Res Care, 2020, ]	PubMed: 32727744
MicroRNA-766-3p Contributes to Anti-Inflammatory Responses through the Indirect Inhibition of NF-κB Signaling [Hayakawa K Int J Mol Sci, 2019, 20(4)]	PubMed: 30769772
Lipocalin-2 derived from adipose tissue mediates aldosterone-induced renal injury. [ JCI Insight, 2018, 3(17)]	PubMed: 30185654

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。