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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

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。
Cas No.1315449-72-9
别名LCI699 phosphate
分子式C13H13FN3O4P
分子量325.23
溶解度H2O : ≥ 200 mg/mL (614.95 mM)
储存条件4°C, away from moisture
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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

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].

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].

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.