mineralocorticoid receptor

Finerenone (BAY-948862) is a nonsteroidal antagonist of the mineralocorticoid receptor (MR) (IC50=18 nM) with selective and oral activity. Finerenone is used in the treatment of patients with chronic kidney disease with type 2 diabetes.

Dicirenone (SC26304) inhibits the Mineralocorticoid receptor (MR), aldosterone regulation of the urinary K+:Na+ ratio, and aldosterone binding to renal cytoplasmic and nuclear receptors.

Apararenone (MT-3995) is a mineralocorticoid receptor antagonist indicated for the treatment of non-alcoholic steatohepatitis and diabetic nephropathy.

Fludrocortisone (Florinef) is a synthetic corticosteroid with moderate glucocorticoid potency and greater mineralocorticoid potency. Fludrocortisone is in research use for the treatment of hypotension.[3]

Eplerenone (CGP 30083) is an aldosterone receptor antagonist and potassium-sparing diuretic used in the therapy of hypertension. Eplerenone therapy has been associated with transient elevations in serum aminotransferase levels, but has yet to be linked to cases of clinically apparent drug induced liver disease.

Fluticasone propionate (CCI-187881), derived from fluticasone used to remedy asthma and allergic rhinitis, is a high affinity, selective GR (glucocorticoid receptor) agonist.

Nimodipine (BAY-e 9736), a 1, 4-dihydropyridine calcium channel blocker, acts primarily on vascular smooth muscle cells.

Spironolactone (SC9420) is an Aldosterone Antagonist. The mechanism of action of spironolactone is as an Aldosterone Antagonist.

Drospirenone (ZK 3059) is a synthetic spironolactone analogue and progestin with progestational and anti-mineralocorticoid activity.

Deoxycorticosterone acetate (DOCA) is a steroid hormone produced by the adrenal glands, possessing mineralocorticoid activity and serving as a precursor to aldosterone. As an agonist of the mineralocorticoid receptor, DOCA can induce severe kidney damage, including inflammation, fibrosis, glomerular injury, and proteinuria. It is commonly used to establish animal models of chronic kidney injury and hypertension.

Canrenoate potassium (Soldactone) is a synthetic pregnadiene derivative with anti-aldosterone activity.

Canrenone (SC14266) is an aldosterone antagonist with potassium-sparing diuretic activity.

Esaxerenone (XL-550) is a highly potent and selective non-steroidal antagonist of the mineralocorticoid receptor.

PF-3882845 is an orally available and selective salicorticoid receptor (MR) antagonist that binds to the progesterone receptor (PR) and can be used to study endocrine diseases and urogenital disorders.

Fludrocortisone acetate (9α-Fludrocortisone acetate), a glucocorticoid-receptor agonist, binds to cytoplasmic receptors, translocates to the nucleus, and initiates transcription of glucocorticoid-responsive genes like lipocortins to inhibit phospholipase A2 (PLA2). As the acetate salt of a synthetic fluorinated corticosteroid, it exhibits anti-inflammatory and antiallergic activities. PLA2 inhibition prevents arachidonic acid release, a precursor of eicosanoids such as prostaglandins and leukotrienes, which are key mediators in the pro-inflammatory response. As a mineralocorticoid-receptor agonist, it stimulates Na+ reabsorption, water retention, and K+ and H+ secretion in the distal tubules and collecting ducts of the kidney.

Vamorolone (VBP15) is an orally active dissociative steroidal anti-inflammatory drug and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone displays effective NF-κB inhibition and substantially decreases hormonal effects.

ZK 216348 is a non-steroidal selective glucocorticoid receptor agonist with an IC50 of 20.3 nM. ZK 216348 also binds to progesterone receptors and mineralocorticoid receptors with IC₅₀ values of 20.4 nM and 79.9 nM, respectively, and may be useful for studying inflammatory bowel disease (IBD).

Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase (CYP11B1) and aldosterone synthase (CYP11B2) with IC50 values ​​of 2.5 and 0.7 nM, respectively, and has been approved by the FDA for the treatment of Cushing's disease.

AZD9977 is a novel, selective modulator of mineralocorticoid receptor .

Ecdysone is a major steroid hormone in insects and herbs. Ecdysone triggers mineralocorticoid receptor activation and induces cellular apoptosis. Ecdysone signaling through Ecdysone receptor isoform B1 is required cell autonomously for the muscle death.

Deoxycorticosterone (Desoxycortone) is a steroid metabolite produced by the adrenal gland. Deoxycorticosterone is an aldosterone precursor and possesses mineralocorticoid activity.

KB-74935 is an enzyme inhibitor and a mineralocorticoid receptor antagonist used to treat cholesterol, hypolipidemia, neurological disorders, and Alzheimer's disease.

RU 26752 is a mineralocorticoid receptor antagonist. It effectively prevents aldosterone-induced hypertension in rats.

mineralocorticoid receptor (MR) antagonist