Aldosterone and cortisol, two significant adrenal steroids, act physiologically through the nuclear receptor superfamily's mineralocorticoid receptor (MR), an intracellular steroid hormone receptor. The glucocorticoid receptor (GR) and the mineralocorticoid receptor (MCR) are closely related, and MCR can bind both MCR and GR hormones indifferently. Aldosterone, the mineralocorticoid receptor's ligand, plays a critical role in sodium reabsorption and blood pressure regulation by activating the mineralocorticoid receptor in the distal nephron. Aldosterone and the human mineralocorticoid receptor tandem also play significant regulatory roles in the cardiovascular and nervous systems in addition to controlling blood pressure and sodium balance.
In sodium-transporting tight epithelia, including the distal nephron, colon, lung, salivary and sweat glands, mineralocorticoid receptor plays a role in the regulation of hydroelectrolytic homeostasis. The enzyme 11-hydroxysteroid dehydrogenase 2 (11-HSD2), which transforms active glucocorticoids into inactive metabolites, provides the mineralocorticoid specificity of aldosterone action in such epithelial target cells. Additionally, non-epithelial tissues like the heart, certain regions of the brain, large blood vessels, and mononuclear leukocytes express the mineralocorticoid receptor. After interacting with the consensus glucocorticoid response element (GRE) sequences, the ligand-activated mineralocorticoid receptor is translocated in the nucleus and functions as a transcription factor. The target genes of the mineralocorticoid receptor may either be activated or have their transcription inhibited.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V4696 | Apararenone | 945966-46-1 | Apararenone (formerly known as MT-3995) is a novel, potent and selective non-steroidalmineralocorticoid/aldosterone receptorantagonist under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis. |
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V20709 | Esaxerenone | 1632006-28-0 | Esaxerenone, formerly known as CS-3150, XL-550, is a nonsteroidal antimineralocorticoid which was discovered by Exelixis and is now under development by Daiichi Sankyo Company for the treatment of hypertension, essential hypertension, hyperaldosteronism, and diabetic nephropathies. |
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V15818 | Finerenone (BAY94-8862) | 1050477-31-0 | Finerenone (formerly known as BAY94-8862;BAY-948862; Kerendia) is a potent, selective, and orally bioavailable non-steroidal anti-mineralocorticoid ormineralocorticoid receptor (MR) antagonist (IC50 = 18 nM) that was approved in July 2021 by the US FDA to reduce the risk of kidney and heart complications in chronic kidney disease associated with type 2 diabetes. |
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