Osilodrostat phosphate (Synonyms: LCI699 phosphate) |
| Catalog No.GC66454 |
El fosfato de osilodrostato (LCI699) es un potente inhibidor de la 11β-hidroxilasa (CYP11B1), activo por vÍa oral, con un valor IC50 de 35 nM. El fosfato de osilodrostat es un potente inhibidor de la aldosterona sintasa (CYP11B2) administrado por vÍa oral con valores IC50 de 0,7 nM y 160 nM para la aldosterona sintasa humana y la aldosterona sintasa de rata, respectivamente. El fosfato de osilodrostato inhibe la sÍntesis de aldosterona y corticosterona. El fosfato de osilodrostat tiene la capacidad de reducir la presiÓn arterial. El fosfato de osilodrostat se puede utilizar para la investigaciÓn del sÍndrome de Cushing (CS).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1315449-72-9
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
IC50: 35 nM (CYP11B1), 0.7 nM (human aldosterone synthase), and 160 nM (rat aldosterone synthase)[1][2]
Osilodrostat (LCI699) phosphate is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat phosphate is a potent, orally aldosterone synthase (CYP11B2) inhibitor with IC50 values 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. |
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *