CORT 118335 (Miricorilant, C118335) is a novel potent, selective, non-steroidal glucocorticoid receptor (GR) antagonist with Ki of 8 nM, shows modest affinity for MR.
RU 752 is a potent mineralocorticoid receptors (type I or MR) antagonist[1].
Esaxerenone is a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist.
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].
(S)-Baxdrostat is the S-enantiomer of Baxdrostat. Baxdrostat is an aldosterone synthase inhibitor[1].
Baxdrostat is a aldosterone synthase inhibitor[1].
Ocedurenone is a corticosteroid receptor antagonist. Ocedurenone can be used for the research of kidney disease (WO2018054357, compound I)[1].
18-Oxocortisol is a derivative of cortisol that is produced by aldosterone synthase (CYP11B2). 18-Oxocortisol is a naturally occurring mineralocorticoid agonist. 18-Oxocortisol is a biomarker in adrenal vein sampling[1][2][3].
Canrenoate (Aldadiene) potassium, a prodrug 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].
Oxprenoate potassium is a potent mineralocorticoid (MR) antagonist. Oxprenoate potassium accentuates DEX (dexamethasone)-induced apoptosis[1].
Deoxycorticosterone acetate is a steroid hormone produced by the adrenal gland that possesses mineralocorticoid activity and acts as a precursor to aldosterone.
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].
SC26304 inhibits the effects of Aldosterone on urinary K+:Na+ ratios and the binding of [3H]Aldosterone to renal cytoplasmic and nuclear receptors.
Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively.
Eplerenone is an aldosterone antagonist with an IC50 of 0.36 μM.Target: Mineralocorticoid ReceptorEplerenone is a selective mineralocorticoid receptor antagonist, which has been shown to produce sustained increases in plasma renin and serum aldosterone, consistent with inhibition of the negative regulatory feedback of aldosterone on renin secretion. The resulting increased plasma renin activity and aldosterone circulating levels do not overcome the effects of eplerenone. Eplerenone selectively binds to recombinant human mineralocorticoid receptors relative to its binding to recombinant human glucocorticoid, progesterone and androgen receptors [1]. Benefits of eplerenone therapy over placebo were also observed in several secondary outcomes, including: death from any cause or hospitalization for HF; death from any cause; hospitalization for any reason; or hospitalization for HF [2].
Fludrocortisone Acetate is a synthetic mineralocorticoid, used to control the amount of sodium and fluids in your body. It is used to treat Addison's disease by decreasing the amount of sodium that is lost (excreted) in your urine，also used to increase blood pressure.
Lorundrostat is a aldosterone synthase inhibitor[1].
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].
Fludrocortisone, a synthetic mineralocorticoid with anti-inflammatory activity.
Vamorolone (VBP15) is a first-in-class, orally active dissociative steroidal anti-inflammatory drug and membrane-stabilizer. Vamorolone improves muscular dystrophy without side effects. Vamorolone shows potent NF-κB inhibition and substantially reduces hormonal effects[1][2].
Canrenone (Aldadiene; SC9376; SC14266) is an aldosterone antagonist extensively used as a diuretic agent.
Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.
Osilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat phosphate is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat phosphate inhibits aldosterone and corticosterone synthesis. Osilodrostat phosphate has blood pressure lowering ability. Osilodrostat phosphate can be used for research of Cushing syndrome (CS)[1][2][3].