エプレレノン
Based on 8 publication(s) in Google Scholar
Eplerenone (Epoxymexrenone) is a selective, highly specific and orally active aldosterone blocker (SAB). Eplerenone also is a selective mineralocorticoid receptor antagonist (MRA) with IC50 value of 0.081 μM. Eplerenone can be used for the research of hypertension, atherosclerosis, chronic systolic heart failure (HF) and cardiovascular (CV).
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 : 99.81%
- CAS 番号: 107724-20-9
- 分子式: C24H30O6
- 分子量:414.49
-
保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
生物活性
-
化学情報
-
溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
-
HY-B0561
SpironolactoneAldosterone/Corticoid Receptor/Androgen Antagonists -
HY-111372
FinerenoneMineralocorticoid Receptor Antagonist -
HY-113313
AldosteroneMineralocorticoid Steroid -
HY-B0251R
Eplerenone (Standard) -
HY-B1618
CorticosteroneEndogenous Glucocorticoids -
HY-B1472
Deoxycorticosterone acetateMineralocorticoid Receptor Agonist -
HY-100471
EsaxerenoneMineralocorticoid Antagonist -
HY-10219
RapamycinmTOR Inhibitor -
HY-13600
Clobetasol propionateCYP3A5 Inhibitor -
HY-18739
Phorbol 12-myristate 13-acetatePKC Activator -
HY-15149
RomidepsinHDAC Inhibitor -
HY-13683
MifepristoneProgesterone Receptor Antagonist
MedChemExpress（MCE）の使用を引用している文献 Eplerenone
More- Br J Pharmacol. 2021 Aug;178(15):2976-2997. [Abstract]
- Biochem Pharmacol. 2026 Jul:249:117928. [Abstract]
- Mol Med Rep. 2020 Sep;22(3):1859-1867. [Abstract]
- Sci Rep. 2025 Dec 1;15(1):45756. [Abstract]
- J Pharm Biomed Anal. 2021 Feb 20:195:113870. [Abstract]
- Theriogenology. 2026 Apr 15:255:117836. [Abstract]
- Otol Neurotol. 2024 Jan 1;45(1):e49-e56. [Abstract]
- Research Square Preprint. 2021 Apr.
Customer Validation & Images
-
Cell Imaging/Staining
-
Histological Imaging/Staining
-
Cell Proliferation/Viability Assay
-
Flow Cytometry
-
WB
Endogenous Metabolite アイソフォーム固有の製品をすべて表示
More
生物活性
製品説明
IC50 & Target
IC50: 0.081 μM (human mineralocorticoid receptor) [2]
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A10 | IC50 |
>5000 nM
Compound: 1
|
Inhibition of L-type calcium channel in rat A10 cells assessed as inhibition of depolarization-induced increase in calcium flux after 48 hrs by FLIPR assay
Inhibition of L-type calcium channel in rat A10 cells assessed as inhibition of depolarization-induced increase in calcium flux after 48 hrs by FLIPR assay
|
[PMID: 20408553] |
| COS-1 | IC50 |
1300 nM
Compound: Eplerenone
|
Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay
Antagonist activity at human MR transfected in human COS1 cells after 1 day by luciferase reporter gene assay
|
[PMID: 22074142] |
| COS-1 | IC50 |
1300 nM
Compound: Eplerenone
|
Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay
Antagonist activity at human mineralocorticoid receptor expressed in COS1 cells after 1 day by luciferase reporter gene assay
|
[PMID: 25187277] |
| HEK293 | IC50 |
2600 nM
Compound: Eplerenone
|
Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting
Displacement of [3H]aldosterone from cytosolic human MR expressed in HEK293 cells after 16 hrs by scintillation counting
|
[PMID: 22074142] |
| Huh-7 | IC50 |
135 nM
Compound: 1
|
Antagonist activity at Gal4-fused mineralocorticoid receptor expressed in human HuH7 cells assessed as inhibition of aldosterone-induced receptor activation by luciferase reporter gene assay
Antagonist activity at Gal4-fused mineralocorticoid receptor expressed in human HuH7 cells assessed as inhibition of aldosterone-induced receptor activation by luciferase reporter gene assay
|
[PMID: 20408553] |
| Huh-7 | IC50 |
122 nM
Compound: 1
|
Antagonist activity at mineralocorticoid receptor LBD expressed in human HUH7 cells coexpressing GAL4 by luciferase reporter gene assay
Antagonist activity at mineralocorticoid receptor LBD expressed in human HUH7 cells coexpressing GAL4 by luciferase reporter gene assay
|
[PMID: 20672820] |
| Huh-7 | IC50 |
122 nM
Compound: eplerenone
|
Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay
Antagonist activity at Gal4-tagged mineralocorticoid receptor expressed in human Huh7 cells by luciferase reporter gene assay
|
[PMID: 20672822] |
体外実験
Eplerenone inhibits the human mineralocorticoid receptor with IC50 value of 0.081 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Atherosclerotic apolipoprotein Edeficient (EO) mice[3]
-
Dosage:200 mg/kg
-
Administration:oral, 200 mg/kg/day for 3 months
-
Result:Significantly decreased systolic and diastolic blood pressure by 12% and 11%, respectively.
Decreased serum susceptibility to lipid peroxidation by as much as 26%, and increased serum paraoxonase activity by 28%.
Reduced levels of lipid peroxides, and significantly reduced macrophage oxidation of low-density lipoprotein (LDL) and superoxide ion release.
Significantly reduced the atherosclerotic lesion area.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 107724-20-9
-
性状 Solid
-
分子量 414.49
-
分子式 C24H30O6
-
Color White to off-white
-
SMILES
O=C(CC1)O[C@@]21CC[C@@]3([H])[C@]4([H])[C@H](C(OC)=O)CC5=CC(CC[C@]5(C)[C@@]46[C@H](O6)C[C@@]32C)=O
-
別名
Eplerenone; Epoxymexrenone
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
-
Journal Impact Factor
-
Most Recent
-
Br J Pharmacol
Protopanaxadiol alleviates neuropathic pain by spinal microglial dynorphin A expression following glucocorticoid receptor activation. [Abstract]2021 Aug;178(15):2976-2997. PMID: 33786848 -
Biochem Pharmacol
Tspan4+ fibroblasts facilitate the development of NECSO in myocardial ischemia reperfusion through migrasomes-mediated Tnf-α autocrine and cardiomyocytes aldosterone generation. [Abstract]2026 Jul:249:117928. PMID: 41887336 -
Mol Med Rep
2020 Sep;22(3):1859-1867. PMID: 32582979
Eplerenone purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2020 Sep;22(3):1859-1867. [Abstract]
Eplerenone (1 μM). Mmunoblotting and semi-quantification of p16, p21, p53 and NADP subunits, p47-phox, p67-phox and gp91-phox expression in H9C2 cells. Protein expression levels were normalized to GAPDH.
-
Sci Rep
Activation/inactivation of Tregs mediated by Kv1.3 potassium channels synergistically with exosome secretion to regulate myocardial fibrosis. [Abstract]2025 Dec 1;15(1):45756. PMID: 41326524
Eplerenone purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Dec 1;15(1):45756. [Abstract]
Eplerenone (200 mg/kg/day). Hematoxylin and eosin (H&E) staining was performed to assess cardiomyocyte arrangement and inflammatory infiltration.
-
J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569 -
Theriogenology
Aldosterone regulates in vitro maturation of porcine oocytes derived from small follicles via Wnt/ β-catenin. [Abstract]2026 Apr 15:255:117836. PMID: 41564797
Eplerenone purchased from MedChemExpress. Usage Cited in: Theriogenology. 2026 Apr 15:255:117836. [Abstract]
Representative images of cumulus cell expansion and oocytes with or without polar bodies in the control group and groups treated with different concentrations of EPL (Eplerenone) after in vitro maturation (IVM).
-
Otol Neurotol
Cortisol Sensitizes Cochlear Hair Cells to Gentamicin Ototoxicity Via Endogenous Apoptotic Pathway. [Abstract]2024 Jan 1;45(1):e49-e56. PMID: 38085767
Eplerenone purchased from MedChemExpress. Usage Cited in: Otol Neurotol. 2024 Jan 1;45(1):e49-e56. [Abstract]
Cells were treated with cortisol (50 μmol/l) in combination with different concentrations of RU486 or Eplerenone for 24 hours.
Eplerenone purchased from MedChemExpress. Usage Cited in: Otol Neurotol. 2024 Jan 1;45(1):e49-e56. [Abstract]
HEI-OC1 cells were treated with 50 μmol/l cortisol in combination with 0.1 nmol/l RU486 or 1 μmol/l Eplerenone for 24 hours and then treated with 50 mmol/l GM for 24 hours. apoptosis was assessed by flow cytometry using Annexin V and PI staining kit.
-
溶剤 & 溶解度
体外:
DMSO : 5 mg/mL (12.06 mM; ultrasonic and warming and heat to 60°C; 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)
純度とドキュメンテーション
-
データシート (297 KB)
-
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
-
取扱説明書 (2659 KB)
参考文献
[1]. Myron H Weinberger, et al. Eplerenone, a selective aldosterone blocker, in mild-to-moderate hypertension. Am J Hypertens. 2002 Aug;15(8):709-16. [Content Brief]
[2]. Dhillon, S., Eplerenone: a review of its use in patients with chronic systolic heart failure and mild symptoms. Drugs, 2013. 73(13): p. 1451-62. [Content Brief]
[3]. Shlomo Keidar, et al. Effect of eplerenone, a selective aldosterone blocker, on blood pressure, serum and macrophage oxidative stress, and atherosclerosis in apolipoprotein E-deficient mice. J Cardiovasc Pharmacol. 2003 Jun;41(6):955-63. [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 | 2.4126 mL | 12.0630 mL | 24.1260 mL | 60.3151 mL |
| 5 mM | 0.4825 mL | 2.4126 mL | 4.8252 mL | 12.0630 mL | |
| 10 mM | 0.2413 mL | 1.2063 mL | 2.4126 mL | 6.0315 mL |
Eplerenone 関連分類
HY-B0251 関連分類
Powered by Bioz