化合物Osilodrostat T4277

Product Introduction
Bioactivity


英文名: Osilodrostat

描述: Osilodrostat (LCI699) 是一种有效的人11β-羟化酶和醛固酮合成酶抑制剂，IC50分别值为2.5 和0.7nM。

动物实验: Sixty male and 60 female rats are randomized into single-sex groups to receive daily doses of pasireotide (0.3 mg/kg/day, s.c.), osilodrostat (20 mg/kg/day, p.o.), osilodrostat/pasireotide in combination (low dose, 1.5/0.03 mg/kg/day; mid-dose, 5/0.1 mg/kg/day; or high dose, 20/0.3 mg/kg/day), or vehicle for 13 weeks.

体内活性: Osilodrostat and pasireotide monotherapies can significantly affect in the histology and mean weights of the pituitary and adrenal glands, liver, and ovary/oviduct. Osilodrostat is associated with adrenocortical hypertrophy and hepatocellular hypertrophy. The combination of Osilodrostat with pasireotide ameliorates the liver and adrenal gland changes observed with monotherapy and does not exacerbate any target organ changes. Cmax and AUC(0–24h) of Osilodrostat and pasireotide increase in an approximately dose-proportional manner. Osilodrostat treatment reduces urinary free cortisol in patients with Cushing's disease; 78.9% has normal urinary free cortisol at week 22.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (220.03 mM)


关键字: HAC15 cells | Cushing syndrome | LCI-699 | primary human adrenocortical cell cultures | inhibit | Mineralocorticoid Receptor | LCI 699 | CYP11B2 | CYP11B1 | Inhibitor | Osilodrostat | blood pressure

相关产品: Fluocinonide | AZD9567 | Hydrocortisone 17-butyrate | Actriol | Prednisolone disodium phosphate | Canrenoate potassium | Triamcinolone acetonide | Dexamethasone Phosphate disodium | Dexamethasone acetate | AZD5423

相关库: Fluorochemical Library

化合物Osilodrostat T4277信息由TargetMol中国为您提供，如您想了解更多关于化合物Osilodrostat T4277报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途