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Osilodrostat

Catalog No. T4277 CAS 928134-65-0

Synonyms: LCI699

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

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Osilodrostat, CAS 928134-65-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 43.00
2 mg	In stock	$ 61.00
5 mg	In stock	$ 85.00
10 mg	In stock	$ 126.00
25 mg	In stock	$ 207.00
50 mg	In stock	$ 401.00
100 mg	In stock	$ 597.00
1 mL * 10 mM (in DMSO)	In stock	$ 74.00

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Purity: 99.12%

Purity: 99.10%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Osilodrostat (LCI699) (LCI699) is an effective inhibitor of human 11β-hydroxylase (IC50: 2.5 nM) and aldosterone synthase (IC50: 0.7 nM).
Targets&IC50	Aldosterone synthase:0.7 nM, 11β-hydroxylase (human):IC50: 2.5 nM
In vivo	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.
Animal Research	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.

Synonyms	LCI699
Molecular Weight	227.24
Formula	C13H10FN3
CAS No.	928134-65-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (220.03 mM)

References and Literature

1. Li L, et al. Osilodrostat (LCI699), a potent 11β-hydroxylase inhibitor, administered in combination with the multireceptor-targeted somatostatin analog pasireotide: A 13-week study in rats. Toxicol Appl Pharmacol. 2015 Aug 1;286(3):224-33. 2. Fleseriu M, et al. Osilodrostat, a potent oral 11β-hydroxylase inhibitor: 22-week, prospective, Phase II study in Cushing's disease. Pituitary. 2016 Apr;19(2):138-48.

Related compound libraries

This product is contained In the following compound libraries：

Fluorochemical Library

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Keywords

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

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