- Signaling Pathways
- Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor
- Mineralocorticoid Receptor
Mineralocorticoid Receptor
Mineralocorticoid receptor (MR) is an intracellular steroid hormone receptor, and a member of the nuclear receptor superfamily, that mediates the physiological action of two important adrenal steroids, aldosterone and cortisol. Mineralocorticoid receptor is closely related to the glucocorticoid receptor (GR), and it can indifferently bind mineralocorticoid and glucocorticoid hormones. Activation of the mineralocorticoid receptor in the distal nephron by its ligand, aldosterone, plays an important role in sodium reabsorption and blood pressure regulation. Besides the regulation of sodium balance and the control of blood pressure, aldosterone-human mineralocorticoid receptor tandem also exerts important regulatory functions on the cardiovascular and central nervous systems.
Mineralocorticoid receptor participates in the regulation of hydroelectrolytic homeostasis in sodium-transporting tight epithelia such as distal nephron, colon, lung, and salivary and sweat glands. In such epithelial target cells, the mineralocorticoid specificity of aldosterone action is given by the enzyme 11β-hydroxysteroid dehydrogenase 2 (11-HSD2), which converts active glucocorticoids into inactive metabolites. Mineralocorticoid receptor is also expressed in nonepithelial tissues such as the heart, some areas of the brain, large blood vessels, and mononuclear leukocytes. The ligand-activated mineralocorticoid receptor is translocated in the nucleus and acts as a transcription factor after its interaction with the consensus glucocorticoid response element (GRE) sequences. Mineralocorticoid receptor could activate or inhibit transcription of target genes whose identification is under intense investigation.
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Mineralocorticoid Receptor Inhibitors
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Mineralocorticoid Receptor Antagonists
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Mineralocorticoid Receptor Ligand
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Mineralocorticoid Receptor Related Products (68)
Related Products (68)
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Apararenone
0 ImagesSynonyms: MT-3995Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis. -
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Vicadrostat
0 ImagesSynonyms: BI 690517Vicadrostat (BI 690517) is an orally active aldosterone synthase (aldosterone synthase) inhibitor, with IC50 values of 19 nM, 16 nM, and 18 μM against human, cynomolgus monkey, and rat aldosterone synthase, respectively. Vicadrostat has an in vivo IC50 of 25 nM for aldosterone synthesis. Vicadrostat exhibits high selectivity for cortisol synthase; it reduces aldosterone production and decreases plasma aldosterone levels. Vicadrostat can be used in the research of chronic kidney disease, heart failure, and hypertension. -
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INCB13739
0 ImagesINCB13739 is an orally active, potent, selective and tissue-specific11β-HSD1 (11β-hydroxysteroid dehydrogenase 1) inhibitor, with IC50 values of 3.2 nM (11β-HSD1 enzymatic) and 1.1 nM (11β-HSD1 PBMC), respectively. INCB13739 can be used for type 2 diabetes mellitus (T2DM) and obesity research. -
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Eplerenone (Standard)
0 ImagesSynonyms: Epoxymexrenone (Standard)Eplerenone (Standard) is the analytical standard of Eplerenone. This product is intended for research and analytical applications. 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). -
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- Desoxycorticosterone pivalate
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(S)-Baxdrostat
0 ImagesSynonyms: (S)-CIN-107(S)-Baxdrostat is the S-enantiomer of Baxdrostat. Baxdrostat is an aldosterone synthase inhibitor. -
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Fludrocortisone acetate (Standard)
0 ImagesSynonyms: 9α-Fludrocortisone acetate(Standard); 9α-Fluorcortisol acetate (Standard)Fludrocortisone acetate (Standard) is the analytical standard of Fludrocortisone acetate. This product is intended for research and analytical applications. -
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Spironolactone-d7
0 ImagesCat. No.: HY-B0561SPurity: 99.96%Synonyms: SC9420-d7Spironolactone-d7 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes. -
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Deoxycorticosterone acetate (Standard)
0 ImagesSynonyms: 11-Deoxycorticosterone acetate(Standard); DOC acetate(Standard); Cortexone acetate (Standard)Deoxycorticosterone acetate (Standard) is the analytical standard of Deoxycorticosterone acetate. This product is intended for research and analytical applications. Deoxycorticosterone acetate (DOCA) is an adrenocortin, acts as a precursor to aldosterone. Deoxycorticosterone acetate is a mineralocorticoid receptor agonist. Deoxycorticosterone acetate can cause severe renal injury, including inflammation, fibrosis, glomerular damage, and proteinuria. -
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(Rac)-Finerenone
0 ImagesSynonyms: (Rac)-BAY 94-8862(Rac)-Finerenone ((Rac)-BAY 94-8862) is the racemate of Finerenone. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). -
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PF-3882845
0 ImagesPF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds to progesterone receptor (PR) with the binding IC50 of 310 nM. -
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Spironolactone-d3
0 ImagesCat. No.: HY-B0561S1Purity: 99.82%Synonyms: SC9420-d3Spironolactone-d3 is the deuterium labeled Spironolactone. Spironolactone (SC9420) is an orally active aldosterone mineralocorticoid receptor antagonist with an IC50 of 24 nM. Spironolactone is also a potent antagonist of androgen receptor with an IC50 of 77 nM. Spironolactone promotes autophagy in podocytes. -
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Spironolactone-d6-1
0 ImagesCat. No.: HY-B0561S4Purity: 99.26%Spironolactone-d6-1 is the deuterium labeled Spironolactone (HY-B0561). Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (Ang II)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type II diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca2+ channels to exert antihypertensive effects. -
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Fludrocortisone acetate-d5
0 ImagesCat. No.: HY-B1203ASSynonyms: 9α-Fludrocortisone acetate-d5; 9α-Fluorcortisol acetate-d5Fludrocortisone acetate-d5 is deuterium labeled Fludrocortisone acetate. -
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Finerenone-d5
0 ImagesCat. No.: HY-111372S1Purity: 99.71%Synonyms: BAY 94-8862-d5Finerenone-d5 (BAY 94-8862-d5) is deuterium labeled Finerenone. Finerenone (BAY 94-8862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease. -
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Oxprenoate potassium
0 ImagesSynonyms: RU 28318Oxprenoate (RU 28318) potassium is an orally active, brain-penetrant selective mineralocorticoid receptor antagonist that blocks Aldosterone (HY-113313) signaling through competitive binding to MR, and exhibits anxiolytic and neuroprotective activities, as well as modulates Corticosterone (HY-B1618) levels. Oxprenoate potassium is used in research on hypertension, anxiety disorders, depression, Alzheimer's disease, and glucocorticoid-related neuronal injury. -
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- Canrenone-d6
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Finerenone-d3
0 ImagesCat. No.: HY-111372SCAS No.: 2917530-37-9Synonyms: BAY 94-8862-d3Finerenone-d3 is the deuterium labeled finerenone (HY-111372). Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). Finerenone has the potential for cardiorenal diseases research, such as type 2 diabetes mellitus and chronic kidney disease. -
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Fludrocortisone-d5
0 ImagesCat. No.: HY-B1203SSynonyms: 9α-Fludrocortisone-d5; 9α-Fluorcortisol-d5Fludrocortisone-d5 (9α-Fludrocortisone-d5) is the deuterium labeled Fludrocortisone (HY-B1203). Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency. -
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Eplerenone-13C,d3
0 ImagesCat. No.: HY-B0251S1Synonyms: Epoxymexrenone-13C,d3Eplerenone-13C,d3 (Epoxymexrenone-13C,d3) is 13C labeled Eplerenone. 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). -
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