For research use only. Not for therapeutic Use.
Esaxerenone, also known as CS-3150, is an aldosterone receptor antagonist. Esaxerenone may be potential useful for preventing or treating hypertension or disease caused by hypertension.
| Catalog Number | I006711 |
| CAS Number | 880780-76-7 |
| Synonyms | Esaxerenone; CS-3150; CS 3150; CS3150.;1-(2-hydroxyethyl)-4-methyl-N-(4-(methylsulfonyl)phenyl)-5-(2-(trifluoromethyl)phenyl)-1H-pyrrole-3-carboxamide |
| Molecular Formula | C22H21F3N2O4S |
| Purity | ≥95% |
| Target | aldosterone receptor antagonist |
| Solubility | Soluble in DMSO, not in water |
| Storage | Store at -20C |
| Reference | 1:Xenobiotica. 2016 Dec 12:1-14. doi: 10.1080/00498254.2016.1263766. [Epub ahead of print] Pharmacokinetics, distribution, and disposition of esaxerenone, a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist, in rats and monkeys.Yamada M,Takei M,Suzuki E,Takakusa H,Kotsuma M,Washio T,Murayama N,Inoue SI,Izumi T, PMID: 27866463 DOI: 10.1080/00498254.2016.1263766 </br><span>Abstract:</span> 1. Esaxerenone (CS-3150) is a novel non-steroidal mineralocorticoid receptor antagonist. The pharmacokinetics, tissue distribution, excretion, and metabolism of esaxerenone were evaluated in rats and monkeys. 2. Following intravenous dosing of esaxerenone at 0.1-3 mg/kg, the total body clearance and the volume of distribution were 3.53-6.69 mL/min/kg and 1.47-2.49 L/kg, respectively, in rats, and 2.79-3.69 mL/min/kg and 1.34-1.54 L/kg, respectively, in monkeys. The absolute oral bioavailability was 61.0-127% in rats and 63.7-73.8% in monkeys. 3. After oral administration of [14C]esaxerenone, the radioactivity was distributed widely to tissues, with the exception of a low distribution to the central nervous system. Both in rats and in monkeys, following oral administration of [14C]esaxerenone the main excretion route of the radioactivity was feces. 4. Five initial metabolic pathways in rats and monkeys were proposed to be N-dealkylation, carboxylation, hydroxymethylation, O-glucuronidation, and O-sulfation. The oxidized metabolism was predominant in rats, while both oxidation and glucuronidation were predominant in monkeys. |
