Cort108297,1018679-79-2

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Cort108297

CAS No. : 1018679-79-2

MCE 国际站：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：GPCR/G Protein

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 (1µM) 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 (80 mg/kg QD), Cort108297 (40 mg/kg BID), Mifepristone (30 mg/kg BID), Rosiglitazone (10 mg/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 40 mg/kg BID or Cort108297 80 mg/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) .

相关产品：Dexamethasone  |  Hydrocortisone  |  Mifepristone  |  Corticosterone  |  Medroxyprogesterone acetate  |  Methylprednisolone  |  Prednisone  |  Prednisolone  |  Ciclesonide  |  Budesonide  |  Cortisone  |  Triamcinolone  |  Flunisolide  |  Fluticasone (propionate)  |  Mometasone furoate  |  (20S)-Protopanaxatriol  |  Fluocinolone (Acetonide)  |  Betamethasone  |  Mapracorat  |  AZD9567  |  Exicorilant  |  AZD7594  |  Deflazacort  |  Beclometasone

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪制药及生命科学研究进展，为您提供全球活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。