Osilodrostat

Osilodrostat (LCI699) is a potent, orally active11β-hydroxylase (CYP11B1) inhibitor with an IC50 value of 35 nM. Osilodrostat 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 inhibits aldosterone and corticosterone synthesis. Osilodrostat has blood pressure lowering ability. Osilodrostat can be used for research of Cushing syndrome (CS) [1][2][3].

Product Specifications

CAS Number

[928134-65-0]

Product Name Alternative

LCI699

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Mineralocorticoid Receptor

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer; Inflammation/Immunology; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/Osilodrostat.html

Purity

99.90

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C) |Ethanol : 100 mg/mL (ultrasonic)

Smiles

N#CC1=CC=C([C@H]2CCC3=CN=CN32)C(F)=C1

Molecular Formula

C13H10FN3

Molecular Weight

227.24

Precautions

H302, H315, H319, H335

References & Citations

[1]Ménard J, et, al. Aldosterone synthase inhibition: cardiorenal protection in animal disease models and translation of hormonal effects to human subjects. J Transl Med. 2014 Dec 10;12:340.|[2]Creemers SG, et, al. Osilodrostat Is a Potential Novel Steroidogenesis Inhibitor for the Treatment of Cushing Syndrome: An In Vitro Study. J Clin Endocrinol Metab. 2019 Aug 1;104 (8) :3437-3449.|[3]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.