For research use only. Not for therapeutic Use.
Esaxerenone（Cat No.:I006711）is a selective mineralocorticoid receptor antagonist (MRA) used in the treatment of hypertension and heart failure with reduced ejection fraction (HFrEF). It works by blocking the mineralocorticoid receptor, which is activated by aldosterone, a hormone that promotes sodium retention and fluid retention, contributing to high blood pressure and heart failure. By inhibiting this receptor, esaxerenone helps lower blood pressure and reduce fluid buildup, improving heart function. It is a newer agent in the MRA class, with a favorable safety profile and fewer side effects, such as hyperkalemia, compared to older MRAs like spironolactone.
| 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 |
| IUPAC Name | 1-(2-hydroxyethyl)-4-methyl-N-(4-methylsulfonylphenyl)-5-[2-(trifluoromethyl)phenyl]pyrrole-3-carboxamide |
| InChI | InChI=1S/C22H21F3N2O4S/c1-14-18(21(29)26-15-7-9-16(10-8-15)32(2,30)31)13-27(11-12-28)20(14)17-5-3-4-6-19(17)22(23,24)25/h3-10,13,28H,11-12H2,1-2H3,(H,26,29) |
| InChIKey | NOSNHVJANRODGR-UHFFFAOYSA-N |
| SMILES | CC1=C(N(C=C1C(=O)NC2=CC=C(C=C2)S(=O)(=O)C)CCO)C3=CC=CC=C3C(F)(F)F |
| 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. |
