首页 Metabolism Hydroxylase Osilodrostat
Osilodrostat
编号 T4277     别名: LCI699, LCI699
CAS 928134-65-0     分子式 C13H10FN3     分子量 227.24
靶点: 11β-hydroxylase; aldosterone synthase;
Osilodrostat (LCI699) is an effective inhibitor of human 11β-hydroxylase (IC50: 2.5 nM) and aldosterone synthase (IC50: 0.7 nM).
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规格 库存 单价 数量
1 mg 上海现货 722.00
2 mg 上海现货 1012.00
5 mg 上海现货 1962.00
10 mg 上海现货 3482.00
25 mg 上海现货 6522.00
50 mg 上海现货 8877.00
100 mg 上海现货 14367.00
1 mL * 10 mM (in DMSO) 上海现货 1962.00
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生物活性

产品描述

Osilodrostat (LCI699) is an effective inhibitor of human 11β-hydroxylase (IC50: 2.5 nM) and aldosterone synthase (IC50: 0.7 nM).

靶点活性

11β-hydroxylase,

aldosterone synthase,

体外活性

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.

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.

化学信息

分子量

227.24

分子式

C13H10FN3

CAS

928134-65-0

溶解度

DMSO: 83.3 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 4.401 ml 22.003 ml 44.006 ml
5 mM 0.88 ml 4.401 ml 8.801 ml
10 mM 0.44 ml 2.2 ml 4.401 ml
50 mM 0.088 ml 0.44 ml 0.88 ml
相关化合物库
本产品收录于以下化合物库中:
  • 经典已知活性库
  • 临床期小分子药物库
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