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Osilodrostat phosphate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Osilodrostat phosphate图片
CAS NO:1315449-72-9
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
LCI699 phosphate
产品介绍
Osilodrostat (LCI699) phosphate 是一种口服有效的 11β-羟化酶 (CYP11B1) 抑制剂,其IC50值为 35 nM。Osilodrostat phosphate 是一种口服有效的醛固酮合成酶 (CYP11B2) 抑制剂,抑制人醛固酮合成酶和大鼠醛固酮合成酶的IC50分别为 0.7 nM 和 160 nM。Osilodrostat phosphate 抑制醛固酮和皮质酮的合成。Osilodrostat phosphate 具有降低血压的能力。Osilodrostat phosphate 可用于库欣综合征 (CS) 的研究。
生物活性

Osilodrostat (LCI699) phosphate is a potent, orallyactive11β-hydroxylase (CYP11B1)inhibitor with anIC50value of 35 nM. Osilodrostat phosphate is a potent, orallyaldosterone synthase (CYP11B2)inhibitor withIC50values of 0.7 nM and 160 nM for human aldosterone synthase and rat aldosterone synthase, respectively. Osilodrostat phosphate inhibits aldosterone and corticosterone synthesis. Osilodrostat phosphate has blood pressure lowering ability. Osilodrostat phosphate can be used for research of Cushing syndrome (CS)[1][2][3].

IC50& Target

IC50: 35 nM (CYP11B1), 0.7 nM (human aldosterone synthase), and 160 nM (rat aldosterone synthase)[1][2]

体外研究
(In Vitro)

Osilodrostat (LCI699; 0.01-10 μM; HAC15 cells, 17 primary human adrenocortical cell cultures, and pituitary adenoma cells) phosphate inhibits cortisol and aldosterone. Osilodrostat results in inhibition of corticosterone, 11-deoxycortisol accumulation, and modest effects on adrenal androgens[2].

体内研究
(In Vivo)

Osilodrostat (LCI699; 0.1-100 mg/kg; p.o.; once) phosphate inhibits aldosterone and corticosterone synthesis in Ang-II- and ACTH-stimulated Sprague Dawley rats[1].
Osilodrostat (LCI699; 3-100 mg/kg; p.o.; daily, for 52 weeks) phosphate reduces mean arterial pressure and prolongs survival in dTG rats[1].

Animal Model:Male Ang-II- and ACTH-stimulated Sprague Dawley rats[1]
Dosage:0.1, 0.3, 1 and 3 mg/kg (Ang-II-stimulated rats) and 1, 3, 10, 30 and 100 mg/kg (ACTH-stimulated rats)
Administration:Oral administration; once
Result:Inhibited the increase in plasma aldosterone concentrations stimulated by Ang II or ACTH in a dose-dependent manner.
Animal Model:dTG rats[1]
Dosage:3, 10, 30 and 100 mg/kg
Administration:Oral administration; daily, for 52 weeks
Result:Increased fractional LV (systolic and diastolic) shortening, normalized LV isovolumic relaxation time to RR (IVRT/RR) ratio and myocardial cell size and reduced LV weight in a dose-dependent manner.
Clinical Trial
分子量

325.23

性状

Solid

Formula

C13H13FN3O4P

CAS 号

1315449-72-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

H2O : ≥ 200 mg/mL(614.95 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.0747 mL15.3737 mL30.7475 mL
5 mM0.6149 mL3.0747 mL6.1495 mL
10 mM0.3075 mL1.5374 mL3.0747 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。