Fludrocortisone (Florinef) is a synthetic corticosteroid with moderate glucocorticoid potency and much greater mineralocorticoid potency. Fludrocortisone can be used to studies on treating low blood pressure.

Osilodrostat (LCI699) (LCI699) is an effective inhibitor of human 11β-hydroxylase (IC50: 2.5 nM) and aldosterone synthase (IC50: 0.7 nM).

Finerenone (BAY-948862) is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist with IC50 of 18 nM for the treatment of chronic heart failure. Finerenone (BAY-948862) displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).

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

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

Apararenone (MT-3995) is a receptor antagonist of mineralocorticoid receptor which can be used to treat non-alcoholic steatohepatitis and diabetic nephropathy.

18-Oxocortisol is a cortisol derivative generated by aldosterone synthase (CYP11B2). It acts as a naturally occurring mineralocorticoid agonist and serves as a biomarker in adrenal vein sampling.

Rac-Finerenone, also known as (Rac)-BAY 94-8862, is the racemate derivative of Finerenone, a selective third-generation nonsteroidal mineralocorticoid receptor antagonist (MR) that is taken orally. With an IC50 value of 18 nM, Finerenone exhibits exceptional selectivity against the glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold).

AZD9977 is a novel, selective modulator of mineralocorticoid receptor .

Spirorenone is an androstadienone derivative as a highly effective aldosterone antagonist. Spirorenone is 8.6 times as potent as spironolactone, but showed a lower affinity for the mineralocorticoid receptors. In phase I clinical trials Spirorenone was absorbed with a half-life of 20-30 min, achieving maximum concentrations of about 100 ng/ml (10 mg) and 260 ng/ml (40 mg) after 1-2 h. Disposition of the parent drug was biphasic with half-lives of 50-60 min (distribution) and 5-6 h (elimination). Neither significant accumulation nor enzyme induction was observed after prolonged treatment.

Oxprenoate Free Base is a mineralocorticoid receptor (MR) antagonist, inhibiting aldosterone production and secretion.

Deoxycorticosterone acetate (Cortexone acetate) is the 21-acetate derivative of desoxycorticosterone, used for intramuscular injection for replacement therapy of the adrenocortical steroid.

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

ZK 216348 also binds to Progesterone and mineralocorticoid receptors (IC50s: 20.4 nM and 79.9 nM, respectively). ZK 216348 is a nonsteroidal selective glucocorticoid receptor agonist (IC50: 20.3 nM). ZK 216348 has an anti-inflammatory activity similar to

Vinclozolin M2, an active metabolite of vinclozolin, is generated through successive esterase activity and decarboxylation in C. elegans, as well as decarboxylation in human liver microsomes. It functions as an antagonist to the mineralocorticoid (IC50= 1,400 nM) and androgen receptors (IC50= 0.17 nM), demonstrated in reporter assays with MCF-7 cells. This compound is exclusively sold for research and analytical purposes, tailored for controlled laboratory use, and is not available in bulk sizes.

Hydrocortisone-d4 is a deuterated compound of Hydrocortisone. Hydrocortisone has a CAS number of 50-23-7. Hydrocortisone, a glucocorticoid receptor agonist, promotes protein catabolism, gluconeogenesis, capillary wall stability, renal excretion of calcium, and suppresses immune and inflammatory responses. Therapeutic Hydrocortisone is a synthetic or semisynthetic analog of natural hydrocortisone hormone produced by the adrenal glands with primary glucocorticoid and minor mineralocorticoid effects.

RU 752 is an antagonist of mineralocorticoid receptor that inhibits aldosterone synthesis.

mineralocorticoid receptor (MR) antagonist

21-hydroxy Eplerenone is a major metabolite of the mineralocorticoid receptor antagonist eplerenone . It is formed from eplerenone by the cytochrome P450 (CYP) isoform CYP3A4.

11-Dehydrocorticosterone is an endogenous mineralocorticoid. It increases Na+/K+-ATPase mRNA expression in vascular smooth muscle cells and inhibits aldosterone action in B. marinus toad bladder tissue in a concentration-dependent manner. 11-Dehydrocorticosterone decreases the sodium/creatine ratio and increases the potassium/creatine ratio in rat urine in a dose-dependent manner in a model of 11β-hydroxysteroid dehydrogenase inhibition induced by carbenoxolone. Chronic administration 11-dehydrocorticosterone increases plasma glucocorticoids levels, body weight gain, and adiposity, as well as induces insulin resistance in mice.

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

Finerenone-d5 is a deuterated compound of Finerenone. Finerenone has a CAS number of 1050477-31-0. Finerenone is a third-generation, selective, and orally available nonsteroidal mineralocorticoid receptor (MR) antagonist with IC50 of 18 nM for the treatment of chronic heart failure. Finerenone displays excellent selectivity versus glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (>500-fold). 

Prorenoate is a steroidal aldosterone antagonist with potassium-sparing diuretic activity. Prorenoate antagonizes the activity of aldosterone at the mineralocorticoid receptor in the nephron and thereby prevents sodium reabsorption. This interferes with the sodium/potassium exchanger and causes sodium and water excretion while reducing potassium excretion.

PF-3882845 also binds to the progesterone receptor (the binding IC50: 310 nM). PF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy.

Aldosterone 21-sulfate is a metabolite of the steroid hormone aldosterone .1It reduces the sodium-to-potassium ratio in rat urine when administered at doses ranging from 10 to 100 μg, indicating mineralocorticoid activity that is less than 1% that of aldosterone.2 1.Grose, J.H., Nowaczynski, W., Kuchel, O., et al.Isolation of aldosterone urinary metabolites, glucuronides and sulfateJ. Steroid Biochem.4(6)551-566(1973) 2.Jowett, T.P., and Slater, J.D.H.Aldosterone 21-sulphate in manJ. Steroid. Biochem.18(4)471-479(2019)

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

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

Budesonide-d8 is a deuterated compound of Budesonide. Budesonide has a CAS number of 51333-22-3. Budesonide, an anti-inflammatory corticosteroid, has shown the effective glucocorticoid activitie and few mineralocorticoid activities. According to reports, Budesonide has extensively inhibitory effects against multiple cells types and mediators referred to allergic and nonallergic-mediated inflammatory. What's more, the anti-inflammatory action of budesonide has been revealed to contribute to the effectiveness of asthma.

Deoxycorticosterone (DOCP) is a mineralocorticoid and is an analog of deoxycorticosterone. Deoxycorticosterone pivalate is used in the treatment of canine low adrenal cortex hormones.

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

18-Hydroxy-11-deoxy Corticosterone (18-OH-DOC) is a mineralocorticoid produced by the zona fasciculata of the adrenal gland, with its biosynthesis regulated by adrenocorticotropic hormone (ACTH) and angiotensin II. This regulation heightens 18-OH-DOC production in isolated human adrenal glomerulosa cells and allows for its formation from 11-deoxy corticosterone (DOC) in human SK-MEL188 melanoma cells. As an intermediate in progesterone metabolism, 18-OH-DOC can be converted to aldosterone in rat adrenal glands' capsular portion. Its continuous infusion (200 μg/rat per day) has been shown to raise systolic blood pressure in uninephrectomized saline-drinking rats, and elevated plasma levels of 18-OH-DOC have been observed in the adb/db mouse model of type 2 diabetes.

6β-hydroxy Eplerenone is a major metabolite of the mineralocorticoid receptor antagonist eplerenone .1 It is formed from eplerenone by the cytochrome P450 (CYP) isoform CYP3A4. |1. Cook, C.S., Berry, L.M., Kim, D.H., et al. Involvement of CYP3A in the metabolism of eplerenone in humans and dogs: Differential metabolism by CYP3A4 and CYP3A5. Drug Metab. Dispos. 30(12), 1344-1351 (2002).

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.

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

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

Aldosterone is the primary mineralocorticoid. Aldosterone is synthesized and secreted in response to renin-angiotensin system activation or high dietary potassium by the zona glomerulosa of the adrenal cortex.

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.

11-Deoxycorticosterone-d8 is a deuterated compound of 11-Deoxycorticosterone. 11-Deoxycorticosterone has a CAS number of 64-85-7. Deoxycorticosterone is a steroid metabolite produced by the adrenal gland. Deoxycorticosterone is an aldosterone precursor and possesses mineralocorticoid activity.

Dexamethasone sodium succinate is the acetate salt form of dexamethasone, which is a synthetic glucocorticoid; it combines high anti-inflammatory effects with low mineralocorticoid activity. At high doses (e.g. 40 mg), it reduces the immune response. Dexamethasone acetate (NEOFORDEX®) is indicated in adults for the treatment of symptomatic multiple myeloma in combination with other medicinal products. Dexamethasone has been shown to induce multiple myeloma cell death (apoptosis) via a down-regulation of nuclear factor-κB activity and an activation of caspase-9 through second mitochondria-derived activator of caspase (Smac; an apoptosis promoting factor) release. Prolonged exposure was required to achieve maximum levels of apoptotic markers along with increased caspase-3 activation and DNA fragmentation. Dexamethasone also down-regulated anti apoptotic genes and increased IκB-alpha protein levels. Dexamethasone apoptotic activity is enhanced by the combination with thalidomide......

11alpha-Hydroxyprogesterone, an inactive analogue of 11beta-Hydroxyprogesterone, serves as an experimental control. Meanwhile, 11beta-Hydroxyprogesterone functions as a potent inhibitor of 11β-Hydroxysteroid dehydrogenase and activates the human mineralocorticoid receptor in COS-7 cells, with an effective dose (ED)50 of 10 nM.

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.

Cortisol-1,2-d2 is a deuterated compound of Cortisol. Cortisol has a CAS number of 50-23-7. Hydrocortisone, a glucocorticoid receptor agonist, promotes protein catabolism, gluconeogenesis, capillary wall stability, renal excretion of calcium, and suppresses immune and inflammatory responses. Therapeutic Hydrocortisone is a synthetic or semisynthetic analog of natural hydrocortisone hormone produced by the adrenal glands with primary glucocorticoid and minor mineralocorticoid effects.