Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 313 | 现货 | ||
2 mg | ¥ 455 | 现货 | ||
5 mg | ¥ 689 | 现货 | ||
10 mg | ¥ 1,070 | 现货 | ||
25 mg | ¥ 1,730 | 现货 | ||
50 mg | ¥ 2,590 | 现货 | ||
100 mg | ¥ 3,980 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 723 | 现货 |
产品描述 | Osilodrostat (LCI699) (LCI699) is an effective inhibitor of human 11β-hydroxylase (IC50: 2.5 nM) and aldosterone synthase (IC50: 0.7 nM). |
靶点活性 | Aldosterone synthase:0.7 nM, 11β-hydroxylase (human):IC50: 2.5 nM |
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. |
别名 | LCI699 |
分子量 | 227.24 |
分子式 | C13H10FN3 |
CAS No. | 928134-65-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (220.03 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.4006 mL | 22.0032 mL | 44.0063 mL | 110.0158 mL |
5 mM | 0.8801 mL | 4.4006 mL | 8.8013 mL | 22.0032 mL | |
10 mM | 0.4401 mL | 2.2003 mL | 4.4006 mL | 11.0016 mL | |
20 mM | 0.22 mL | 1.1002 mL | 2.2003 mL | 5.5008 mL | |
50 mM | 0.088 mL | 0.4401 mL | 0.8801 mL | 2.2003 mL | |
100 mM | 0.044 mL | 0.22 mL | 0.4401 mL | 1.1002 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Osilodrostat 928134-65-0 Endocrinology/Hormones Metabolism Others Glucocorticoid Receptor Hydroxylase HAC15 cells Cushing syndrome LCI-699 primary human adrenocortical cell cultures inhibit Mineralocorticoid Receptor LCI 699 CYP11B2 CYP11B1 Inhibitor blood pressure LCI699 inhibitor