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Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat 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.
In HAC15 cells, osilodrostat inhibited cortisol production more potently (IC50 = 0.035 µM).
| Molecular Weight | 227.24 |
| Formula | C13H10FN3 |
| CAS Number | 928134-65-0 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL Ethanol 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Mineralocorticoid Receptor Products |
|---|
| Spironolactone
Spironolactone (SC9420) is an oral active aldosterone mineralocorticoid receptor antagonist with an IC50 value of 24 nM. Spironolactone is also an androgen receptor antagonist with an IC50 of 77 nM. Spironolactone promotes podocyte autophagy. |
| Potassium canrenoate
Canrenoate potassium is a predrug for the release of Canrenone and an effective antagonist of competitive salt ocorticoid receptor. As a diuretic, Canrenoate potassium is used in the study of hypertension. |
| Canrenone
Canrenone is a mineralocorticoid receptor antagonist. |
| Finerenone
Finerenone (BAY 94-8862) is a third generation selective, oral active, non-steroidal halocorticoid receptor (MR) antagonist (IC50=18 nM). Finerenone showed good selectivity (>500-fold) compared to glucocorticoid receptor (GR), androgen receptor (AR), and progesterone receptor (AR). Finerenone has potential applications in the study of heart and kidney diseases, such as type 2 diabetes and chronic kidney disease. |
| Esaxerenone (CS-3150)
Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist. |
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