Description
Esaxerenone (CS-3150) is a highly potent and selective non-steroidal mineralocorticoid receptor antagonist.
Product information
CAS Number: 1632006-28-0
Molecular Weight: 466.47
Formula: C22H21F3N2O4S
Chemical Name: 1-(2-hydroxyethyl)-N-(4-methanesulfonylphenyl)-4-methyl-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide
Smiles: CC1C(=CN(CCO)C=1C1=CC=CC=C1C(F)(F)F)C(=O)NC1=CC=C(C=C1)S(C)(=O)=O
InChiKey: NOSNHVJANRODGR-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (214.38 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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