| Identification | Back Directory | [Name]
Esaxerenone | [CAS]
1632006-28-0 | [Synonyms]
cs3150
cs-3150
XL-550)
CS-2614
Esaxerenone
5G,100G,500G
CS-3150
(Esaxerenone
CS-3150; CS 3150; CS3150; XL-550; XL550; XL 550.
1H-Pyrrole-3-carboxamide, 1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-, (5S)- | [Molecular Formula]
C22H21F3N2O4S | [MDL Number]
MFCD31630843 | [MOL File]
1632006-28-0.mol | [Molecular Weight]
466.47 |
| Chemical Properties | Back Directory | [Boiling point ]
581.3±50.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [solubility ]
DMSO:100.0(Max Conc. mg/mL);214.37(Max Conc. mM) | [form ]
Solid | [pka]
12.76±0.70(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
Esaxerenone, is a novel, highly potent and selective non-steroidal mineralocorticoid receptor antagonist. | [Biological Activity]
Esaxerenone exerts its antihypertensive effect by blocking excessive activation of the mineralocorticoid receptor by endogenous ligands (such as aldosterone), has a mineralocorticoid receptor selectivity at least 1000-fold greater than other steroid hormone receptors, a long half-life, high oral bioavailability, and has a more significant antihypertensive effect than spironolactone or eplerenone. | [Synthesis]
below shows the synthesis route of Esaxerenone
 | [in vivo]
After single oral administration of Esaxerenone at 0.1, 0.3, 1, and 3?mg/kg, maximum plasma concentration (Cmax) and the area under the plasma concentration versus time curve (AUC) are increased with dose. Time to reach the maximum plasma concentration (Tmax) of Esaxerenone ranges from 2.0 to 4.5?h. After intravenous administration of Esaxerenone at 0.1, 0.3, 1, and 3?mg/kg, the total body clearance (CL) and distribution volume at steady state (Vss) are 3.53 to 6.69?mL/min/kg and 1.47 to 2.49?L/kg, respectively, in rats, and 2.79 to 3.69?mL/min/kg and 1.34 to 1.54?L/kg, respectively, in cynomolgus monkeys. Up to 168?h after administration, 3.9% and 91.4% of dosed radioactivity are excreted in rat urine and feces, respectively, and 95.2% in total. In monkeys, the excreted radioactivity up to 168?h is 11.5% in urine, 82.3% in feces, and 93.9% in total[1]. |
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