CS-3150

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CS-3150 (Esaxerenone, XL-550) 是一种高效、选择性、口服活性的非甾体盐皮质激素受体拮抗剂，IC50 为 9.4 nM。

CS-3150 (Esaxerenone, XL-550) is a?highly potent, selective and orally active non-steroidal mineralocorticoid receptor antagonist with IC50 of 9.4 nM; displays >1,000-fold selectivity over other steroid hormone receptors, glucocorticoid receptor, androgen receptor and progesterone receptor; inhibits aldosterone-induced transcriptional activation of human mineralocorticoid receptor with IC50 of 3.7 nM, shows superior potency to that of spironolactone and eplerenone; suppresses aldosterone-induced decrease in urinary Na(+)/K(+) ratio, inhibits blood pressure elevation induced by DOCA/salt-loading in rats.Diabetes Phase 3 Clinical.

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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.

Esaxerenone | XL-550

Nuclear Receptor/Transcription Factor

MLR

MLR

Metabolic Disease

Diabetes

1632006-28-0

466.475

C22H21F3N2O4S

>98% (HPLC)

DMSO : ≥ 125 mg/mL 267.97 mM

CS(C1=CC=C(NC(C2=CN(CCO)C(C3=CC=CC=C3C(F)(F)F)=C2C)=O)C=C1)(=O)=O

(S)-1-(2-Hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl) phenyl]-5-[2-(trifluoromethyl) phenyl]-1H-pyrrole-3-carboxamide

(-20℃)

With Ice Pack

≥ 2 years