1. Signaling Pathways
  2. Metabolic Enzyme/Protease
    Vitamin D Related/Nuclear Receptor
  3. 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.

Mineralocorticoid Receptor Related Products (63):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-120321
    DSR-71167
    Antagonist
    DSR-71167 is an orally active mineralocorticoid receptor (MR) antagonist with an IC50 of 0.26 μM. DSR-71167 exhibits weak carbonic anhydrase (CA) inhibitory activity with an IC50 of 19 μM. DSR-71167 can dose-dependently increase urinary sodium excretion in rat models and has a very low risk of hyperkalemia in potassium-loading rat models. DSR-71167 lowers systolic blood pressure in hypertensive rat models. DSR-71167 can be used for research on hypertension and heart failure.
    DSR-71167
  • HY-Z7760
    Felodipine 3,5-dimethyl ester
    Modulator
    Felodipine 3,5-Dimethyl Ester is a aryldihydropyridine derivatives for use as mineralocorticoid receptor modulator and voltage-dependent L-type calcium channel CaV1.2 inhibitor.
    Felodipine 3,5-dimethyl ester
  • HY-P5458
    SRC-1 (686-700)
    Activator
    SRC-1 (686-700) is a biological active peptide. (This peptide is amino acids 686 to 700 fragment containing the second LXXLL motif, derived from NR box II of steroid receptor coactivator (SRC1). Coactivator proteins interact with nuclear receptors in a ligand-dependent manner and augment transcription.)
    SRC-1 (686-700)
  • HY-117965
    Miricorilant
    Antagonist
    Miricorilant (CORT 118335) is a dual selective glucocorticoid (GR) modulator/mineralocorticoid (MR) antagonist. Miricorilant can be used for the research of hypothalamic-pituitary-adrenal (HPA) axis related disorders.
    Miricorilant
  • HY-B1203R
    Fludrocortisone (Standard)
    Agonist
    Fludrocortisone (Standard) (9α-Fludrocortisone (Standard)) is the analytical standard of Fludrocortisone (HY-B1203). This product is intended for research and analytical applications. 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.
    Fludrocortisone (Standard)
  • HY-B0561S2
    Spironolactone-d3-1
    Antagonist
    Spironolactone-d3-1 is 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.
    Spironolactone-d<sub>3</sub>-1
  • HY-B1203S1
    Fludrocortisone-d2
    Agonist
    Fludrocortisone-d2 (9α-Fludrocortisone-d2) 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.
    Fludrocortisone-d<sub>2</sub>
  • HY-B0251S
    Eplerenone-d3
    Antagonist
    Eplerenone-d3 is the deuterium labeled Eplerenone. Eplerenone (Epoxymexrenone) is a selective, competitive and oreally active aldosterone antagonist with an IC50 of 138 nM. Eplerenone has low affinity for progesterone, androgen, estrogen and glucocorticoid receptors. Eplerenone can be used for hypertension and heart failure after myocardial infarction reserch.
    Eplerenone-d<sub>3</sub>
  • HY-P5950
    ACTH (6-24) (human)
    Inhibitor
    ACTH (6-24) (human) (Adrenocorticotropic hormone (6-24)) is an ACTH fragment. ACTH (6-24) (human) is a competitive inhibitor of steroidogenesis induced by ACTH (1-39) and ACTH (5-24) (Kd:13.4 and 3.4 nM). ACTH (6-24) (human) inhibits corticosterone production and cAMP accumulation induced by hPTH 1-34.
    ACTH (6-24) (human)
  • HY-B1438S1
    Canrenone-d4
    Antagonist
    Canrenone-d4 is deuterium labeled Canrenone. Canrenone (Aldadiene) is an aldosterone antagonist extensively used as a diuretic agent.
    Canrenone-d<sub>4</sub>
  • HY-107630
    RU 26752
    Antagonist
    RU 26752 is a steroid hormone receptor antagonist. RU 26752 can prevent hypertension caused by aldosterone (HY-113313) in rats.
    RU 26752
  • HY-100471R
    Esaxerenone (Standard)
    Antagonist
    Esaxerenone (Standard) is the analytical standard of Esaxerenone. This product is intended for research and analytical applications. Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist.
    Esaxerenone (Standard)
  • HY-109017R
    Vamorolone (Standard)
    Antagonist
    Vamorolone (Standard) is the analytical standard of Vamorolone. This product is intended for research and analytical applications.
    Vamorolone (Standard)
  • HY-W738639
    18-Hydroxy-11-deoxy corticosterone
    Ligand
    18-Hydroxy-11-deoxy corticosterone (18-OH-DOC) is a mineralocorticoid whose synthesis is regulated by adrenocorticotropic hormone (ACTH) and angiotensin II. 18-Hydroxy-11-deoxy corticosterone is an intermediate in the metabolism of progesterone and plays an important role in regulating blood pressure and water-salt balance. Continuous infusion of 18-Hydroxy-11-deoxy corticosterone can increase systolic blood pressure in rats, and plasma levels of 18-Hydroxy-11-deoxy corticosterone are significantly elevated in the db/db mouse model of type 2 diabetes, suggesting its potential involvement in metabolic dysregulation and diabetes-related regulation. 18-Hydroxy-11-deoxy corticosterone holds promise for research in areas such as hypertension, diabetes, and other related fields.
    18-Hydroxy-11-deoxy corticosterone
  • HY-B1438S2
    Canrenone-d7
    Antagonist 99.60%
    Canrenone-d7 (Aldadiene-d7 ) is deuterium labeled Canrenone. Canrenone (Aldadiene) is an aldosterone antagonist extensively used as a diuretic agent.
    Canrenone-d<sub>7</sub>
  • HY-109002R
    Apararenone (Standard)
    Antagonist
    Apararenone (Standard) is the analytical standard of Apararenone (HY-109002). This product is intended for research and analytical applications. Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.
    Apararenone (Standard)
  • HY-16276R
    Osilodrostat (Standard)
    Inhibitor
    Osilodrostat (Standard) is the analytical standard of Osilodrostat. This product is intended for research and analytical applications. Osilodrostat (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).
    Osilodrostat (Standard)
  • HY-163751
    STING-IN-9
    Inhibitor
    STING-IN-9 (compound 2) is a potent inhibitor of human CYP11B2. STING-IN-9 showed more than 80 times higher selectivity over human CYP11B1 in vitro.
    STING-IN-9
  • HY-W749323
    21-Hydroxyeplerenone
    Control
    21-Hydroxyeplerenone is a major metabolite of the mineralocorticoid receptor antagonist Eplerenone (HY-B0251). 21-Hydroxyeplerenone is formed from eplerenone by the cytochrome P450 (CYP) isoform CYP3A4.
    21-Hydroxyeplerenone
  • HY-136969
    RU 752
    Antagonist
    RU 752 is a potent mineralocorticoid receptors (type I or MR) antagonist.
    RU 752