Esaxerenone Chemical Properties

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)

pka

12.76±0.70(Predicted)

form 

Solid

color 

White to light yellow

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

C(N1C=C(C(=O)NC2C=CC(S(=O)(=O)C)=CC=2)C(C)=C1C1C=CC=CC=1C(F)(F)F)CO

Esaxerenone Usage And Synthesis

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