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 Agonists
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Mineralocorticoid Receptor Antagonists
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Mineralocorticoid Receptor Activator
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Mineralocorticoid Receptor Modulators
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Mineralocorticoid Receptor Control
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Mineralocorticoid Receptor Ligand
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Mineralocorticoid Receptor Related Products (65)
Related Products (65)
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Finerenone
0 ImagesSynonyms: BAY 94-8862Finerenone (BAY 94-8862) is a third-generation, selective, and orally active 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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Spironolactone
0 ImagesSpironolactone 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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Eplerenone
0 ImagesSynonyms: EpoxymexrenoneEplerenone (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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Deoxycorticosterone
0 ImagesDeoxycorticosterone is a steroid hormone produced by the adrenal gland that possesses mineralocorticoid activity and acts as an aldosterone precursor. Deoxycorticosterone is an agonist for O. mykiss mineralocorticoid receptor (rtMR) transcription with EC50 of 0.16 nM. Deoxycorticosterone could acts as an immune stimulator in fish.
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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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Esaxerenone-d4
0 ImagesCat. No.: HY-100471SSynonyms: CS-3150-d4; XL-550-d4Esaxerenone-d4 (CS-3150-d4) is the deuterium labeled Esaxerenone (HY-100471). Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist.
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(R)-Finerenone
0 ImagesSynonyms: (R)-BAY 94-8862(R)-Finerenone ((R)-BAY 94-8862) is the R-isomer of Finerenone (HY-111372). Finerenone is a third-generation selective, orally active, non-steroidal mineralocorticoid receptor (MR) antagonist (IC50 = 18 nM). Compared with glucocorticoid receptors (GR), androgen receptors (AR), and progesterone receptors (AR), Finerenone shows good selectivity (> 500-fold). Finerenone has potential application prospects in studies of heart and kidney diseases, such as type 2 diabetes and chronic kidney disease.
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Deoxycorticosterone acetate
0 ImagesSynonyms: 11-Deoxycorticosterone acetate; DOC acetate; Cortexone acetateDeoxycorticosterone 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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Osilodrostat
0 ImagesSynonyms: LCI699Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat inhibits aldosterone and corticosterone synthesis. Osilodrostat has blood pressure lowering ability. Osilodrostat can be used for research of Cushing syndrome (CS).
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Baxdrostat
0 ImagesSynonyms: CIN-107Baxdrostat is a aldosterone synthase inhibitor.
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Fludrocortisone
0 ImagesFludrocortisone (9α-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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Esaxerenone
0 ImagesSynonyms: CS-3150; XL-550Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist.
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Fludrocortisone acetate
0 ImagesSynonyms: 9α-Fludrocortisone acetate; 9α-Fluorcortisol acetateFludrocortisone acetate (9α-Fludrocortisone acetate) is an orally active synthetic mineralocorticoid. Fludrocortisone acetate can effectively control sodium retention. Fludrocortisone acetate is used in studies of cardiac injury, adrenal insufficiency and orthostatic hypotension.
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Spironolactone (Standard)
0 ImagesSpironolactone (Standard) is the analytical standard of Spironolactone. This product is intended for research and analytical applications. 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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Balcinrenone
0 ImagesSynonyms: AZD9977Balcinrenone (AZD9977) is a potent, selective, and orally active mineralocorticoid receptor (MR) modulator. Balcinrenone is used for heart failure, and chronic kidney disease research.
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Osilodrostat phosphate
0 ImagesSynonyms: LCI699 phosphateOsilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat phosphate is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat phosphate inhibits aldosterone and corticosterone synthesis. Osilodrostat phosphate has blood pressure lowering ability. Osilodrostat phosphate can be used for research of Cushing syndrome (CS).
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Ocedurenone
0 ImagesSynonyms: KBP-5074Ocedurenone is a corticosteroid receptor antagonist. Ocedurenone can be used for the research of kidney disease (WO2018054357, compound I).
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Canrenone (Standard)
0 ImagesSynonyms: Aldadiene(Standard); SC9376 (Standard)Canrenone (Standard) is the analytical standard of Canrenone. This product is intended for research and analytical applications. Canrenone (Aldadiene) is an aldosterone antagonist extensively used as a diuretic agent.
