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Esaxerenone

Catalog No.: 1710121
Cas No.: 1632006-28-0
Purity : >98%

Esaxerenone (INN) (developmental code names CS-3150, XL-550) is a nonsteroidal antimineralocorticoid which was discovered by Exelixis and is now under development by Daiichi Sankyo Company for the treatment of hypertension, essential hypertension, hyperaldosteronism, and diabetic nephropathies. It acts as a highly selective silent antagonist of the mineralocorticoid receptor (MR), the receptor for aldosterone, with greater than 1,000-fold selectivity for this receptor over other steroid hormone receptors, and 4-fold and 76-fold higher affinity for the MR relative to the existing antimineralocorticoids spironolactone and eplerenone. As of 2017, esaxerenone is in phase III clinical trials for hypertension, essential hypertension, and hyperaldosteronism and is in phase II clinical trials for diabetic nephropathies.

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Chemical Information

NameEsaxerenone
Iupac Chemical Name1-(2-hydroxyethyl)-4-methyl-N-(4-methylsulfonylphenyl)-5-[2-(trifluoromethyl)phenyl]pyrrole-3-carboxamide
SynonymsEsaxerenone; CS-3150; CS 3150; CS3150.
Molecular FormulaC22H21F3N2O4S
Molecular Weight466.4752
SmileCS(C1=CC=C(NC(C2=CN(CCO)C(C3=CC=CC=C3C(F)(F)F)=C2C)=O)C=C1)(=O)=O
InChiKeyNOSNHVJANRODGR-UHFFFAOYSA-N
InChiInChI=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)
CAS Number1632006-28-0
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Ordering Information

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Formulationoff-white solid
Purity>98%
Storage3 years -20ºCpowder
SolubilitySoluble in DMSO
Handling
Shipping ConditionShipped under ambient temperature as non-hazardous chemical.
HS Code
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study
Not available

Chemical Structure

1710121 - Esaxerenone | CAS 1632006-28-0

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