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Cort108297

CAS No. : 1018679-79-2

MCE 站：Cort108297

产品活性：Cort108297 是一种高亲和性的特异性糖皮质激素受体 (GR) 拮抗剂，K_i 值为 0.45 nM。

研究领域：Immunology/Inflammation  |  Vitamin D Related/Nuclear Receptor

作用靶点：Glucocorticoid Receptor

In Vitro: In LAPC4 cells, co-treatment with Dexamethasone induces steady-state SGK1 expression 1.7-fold compared to R1881/Enzalutamide (RE) treatment alone. Addition of CORT118335 (1M) inhibits Dexamethasone-induced SGK1 expression 50% while Cort108297 completely blocks the Dexamethasone-mediated SGK1 increase (p<0.05). KLK3 expression is increased 2.5-fold by Dexamethasone compared to treatment with RE. Both Cort108297 ａnd CORT118335 antagonize Dexamethasone-induced KLK3 expression (by 48% ａnd 60%, respectively, p<0.05). Following 3 days of Dexamethasone±SGRMs in CWR-22Rv1 cells, SGK1 gene expression is dramatically induced by ~100-fold compared to RE-treated cells ａnd this induction is completely abrogated by both Cort108297 ａnd CORT118335 (p<0.01). KLK3 is also induced (7.5-fold) by Dexamethasone compared to RE in CWR-22Rv1 cells; Cort108297 ａnd CORT118335 inhibits this induction by 70% ａnd 75%, respectively (p<0.01).

In Vivo: Ten-week-old, male, C57BL/6J mice are fed a diet containing 60% fat calories ａnd water supplemented with 11% sucrose for 4 weeks. Groups (n=8) receive one of the following: Cort108297 (80mg/kg QD), Cort108297 (40mg/kg BID), Mifepristone (30mg/kg BID), Rosiglitazone (10mg/kg QD), or vehicle. Compared to mice receiving a high-fat, high-sugar diet plus vehicle, mice receiving a high-fat, high-sugar diet plus either Mifepristone or Cort108297 gain significantly less weight. At the end of the four week treatment period, mice receiving Cort108297 40mg/kg BID or Cort108297 80mg/kg QD also have significantly lower steady plasma glucose than mice receiving vehicle. Male rats are treated for five days with Mifepristone (10 mg/kg), Cort108297 (30 mg/kg ａnd 60 mg/kg), Imipramine (10mg/kg) or vehicle ａnd exposed to forced swim test (FST) or restraint stress. Both doses of Cort108297 potently suppress peak corticosterone responses to FST ａnd restraint stress. However, only the higher dose of Cort108297 (60mg/kg) significantly decreases immobility in the forced swim test (FST) .

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