Mineralocorticoid Receptor

Levonorgestrelis a synthetic progesterone analog; binds to the progesterone receptor (relative binding affinities are < 0.02, 7.5, 17, 58 and 323 % for estrogen receptors, glucocorticoid receptors, mineralocorticoid receptors, androgen receptors and progesterone receptors respectively).

Deoxycorticosterone acetate (DOCA) is a corticosteroid.

Esaxerenone, also known as CS-3150, XL-550, is a nonsteroidal antimineralocorticoid that acts as a highly selective silent antagonist of the mineralocorticoid receptor (MR), the receptor for aldosterone, with greater than 1,000-fold selectivity for this receptor over other steroid hormone receptors, and 4-fold and 76-fold higher affinity for the MR relative to the existing antimineralocorticoids spironolactone and eplerenone.

Canrenone is a metabolite of spironolactone, Na/K ATPase partial agonist and aldosterone and androgen receptor antagonist used as a diuretic.

Deoxycorticosterone is a steroid hormone produced by the adrenal gland that possesses mineralocorticoid activity and acts as an aldosterone precursor.

Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.

DSR-71167 is an orally active mineralocorticoid receptor antagonist exhibiting an IC50 of 0.26 μM. This compound displays weak carbonic anhydrase inhibitory activity with an IC50 of 19 μM. DSR-71167 has demonstrated the ability to dose-dependently enhance urinary sodium excretion and effectively lowers systolic blood pressure in hypertensive rat models, while presenting a low risk of hyperkalemia in potassium-loading scenarios. It is suitable for research focused on hypertension and heart failure.

Finerenone is a selective nonsteroidal mineralocorticoid receptor (MR) antagonist with a reported IC50 of 18 nM. It demonstrates high selectivity against glucocorticoid, androgen, and progesterone receptors, with over 500-fold preference. Finerenone is relevant for researching therapeutic interventions in cardiorenal diseases, particularly in the context of type 2 diabetes mellitus and chronic kidney disease.

Balcinrenone (AZD9977) is a selective, orally active modulator of the mineralocorticoid receptor (MR). It demonstrates significant biological activity in the context of heart failure and chronic kidney disease research. This compound is primarily utilized in studies investigating MR-related pathways and their implications in cardiovascular and renal health.

Felodipine 3,5-Dimethyl Ester is a dihydropyridine derivative functioning primarily as a mineralocorticoid receptor modulator and a selective inhibitor of the voltage-dependent L-type calcium channel CaV1.2. This compound exhibits significant pharmacological activity by affecting calcium ion flux, which plays a crucial role in cardiovascular and renal physiology. Its applications extend to research in hypertension, heart failure, and other cardiovascular disorders related to calcium channel dysregulation.

RU 26752 is a mineralocorticoid receptor antagonist that modulates the activity of steroid hormone receptors. It effectively inhibits hypertension induced by aldosterone in preclinical models, making it a valuable tool for studying cardiovascular diseases and related conditions. This compound is useful for researchers investigating the role of mineralocorticoid receptors in hypertension and its pathophysiological mechanisms.

21-Hydroxyeplerenone is a major metabolite of the mineralocorticoid receptor antagonist Eplerenone, produced through the action of the cytochrome P450 isoform CYP3A4. As a potent mineralocorticoid receptor modulator, it plays a crucial role in regulating blood pressure and electrolyte balance. This compound is useful for research focused on cardiovascular health, renal function, and the therapeutic potential of mineralocorticoid receptor antagonism.

RU 752 is a potent antagonist of mineralocorticoid receptors (MR). It effectively binds to these receptors, inhibiting their activity and modulating mineralocorticoid signaling pathways. This compound has significant potential in research applications related to cardiovascular diseases, hypertension, and disorders associated with excessive mineralocorticoid activity.

Dicirenone is a mineralocorticoid receptor antagonist that inhibits the actions of aldosterone. It effectively reduces urinary potassium to sodium ratios and impedes the binding of [3H]aldosterone to renal cytoplasmic and nuclear receptors. This compound is utilized in research related to hypertension, heart failure, and electrolyte balance.