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 (34):

Cat. No. Product Name Effect Purity
  • HY-111372
    Finerenone Antagonist 99.95%
    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[1][2].
  • HY-B0561
    Spironolactone Antagonist 99.75%
    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[1][2][3].
  • HY-100471
    Esaxerenone Antagonist 99.88%
    Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist[1].
  • HY-16276
    Osilodrostat Inhibitor 99.90%
    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)[1][2][3].
  • HY-109017
    Vamorolone Antagonist 99.12%
    Vamorolone (VBP15) is a first-in-class, orally active dissociative steroidal anti-inflammatory agent and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone shows potent NF-κB inhibition and substantially reduces hormonal effects[1][2].
  • HY-111372A
    (Rac)-Finerenone Antagonist 99.66%
    (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)[1].
  • HY-B1203S
    Fludrocortisone-d5 Agonist
    Fludrocortisone-d5 is the deuterium labeled Fludrocortisone. Fludrocortisone, a synthetic mineralocorticoid with anti-inflammatory activity.
  • HY-B1438
    Canrenone Antagonist 99.83%
    Canrenone (Aldadiene) is an aldosterone antagonist extensively used as a diuretic agent.
  • HY-B1203
    Fludrocortisone Agonist
    Fludrocortisone, a synthetic mineralocorticoid with anti-inflammatory activity.
  • HY-150701
    INCB13739 Inhibitor 99.79%
    INCB13739 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[1].
  • HY-12738
    PF-3882845 Antagonist
    PF-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[1].
  • HY-109002
    Apararenone Antagonist 98.98%
    Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.
  • HY-132827
    Ocedurenone Antagonist
    Ocedurenone is a corticosteroid receptor antagonist. Ocedurenone can be used for the research of kidney disease (WO2018054357, compound I)[1].
  • HY-B1582A
    Canrenoate potassium Antagonist 99.37%
    Canrenoate (Aldadiene) potassium, a proagent that releases canrenone, is a potent, competitive mineralocorticoid receptor (aldosterone receptor) antagonist. Potassium canrenoate, as a diuretic, is used for the research of hypertension[1][2][3].
  • HY-B1472
    Deoxycorticosterone acetate Agonist
    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[1][2].
  • HY-132809
    Baxdrostat Inhibitor 99.60%
    Baxdrostat is a aldosterone synthase inhibitor[1].
  • HY-16276A
    Osilodrostat phosphate Inhibitor 99.35%
    Osilodrostat (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)[1][2][3].
  • HY-147277
    Lorundrostat Inhibitor 99.37%
    Lorundrostat is a aldosterone synthase inhibitor[1].
  • HY-B0561S1
    Spironolactone-d3 Antagonist
    Spironolactone-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[1][2][3].
  • 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[1][2][3].