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 (56):

Cat. No. Product Name Effect Purity
  • HY-111372
    Finerenone Antagonist 99.66%
    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 99.63%
    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[1][2][3][4][5][6][7][8][9][10].
  • 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-109017
    Vamorolone Antagonist 99.10%
    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-113414
    Deoxycorticosterone Agonist 99.61%
    Deoxycorticosterone 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[3]. Deoxycorticosterone could acts as an immune stimulator in fish[4].
  • 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[1].
  • HY-B1438S2
    Canrenone-d7 Antagonist
    Canrenone-d7 (Aldadiene-d7 ) is deuterium labeled Canrenone. Canrenone (Aldadiene) is an aldosterone antagonist extensively used as a diuretic agent.
  • HY-B0251S1
    Eplerenone-13C,d3 Antagonist
    Eplerenone-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)[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-B0561R
    Spironolactone (Standard) Antagonist 98.55%
    Spironolactone (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[1][2][3].
  • HY-B1438
    Canrenone Antagonist 99.56%
    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 99.90%
    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-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.)
  • 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[1].
  • HY-109002
    Apararenone Antagonist 99.09%
    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 99.42%
    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 99.89%
    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].