Osilodrostat (phosphate)

• UNSPSC Description:

  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].

• Target Antigen:

  Mineralocorticoid Receptor

• Type:

  Reference compound

• Related Pathways:

  Metabolic Enzyme/Protease;Vitamin D Related/Nuclear Receptor

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer; Cardiovascular Disease

• Assay Protocol:

  https://www.medchemexpress.com/osilodrostat-phosphate.html

• Solubility:

  H2O : ≥ 200 mg/mL

• Smiles:

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

• Molecular Weight:

  325.23

• 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.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Launched

• CAS Number:

  1315449-72-9