Osilodrostat

• CAT Number: I008509
• CAS Number: 928134-65-0
• Molecular Formula: C13H10FN3
• Molecular Weight: 227.24
• Purity: 95%
• Synonyms: 4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile
• Target: CYP11B1
• Target Protein: P15538
• Appearance: Solid
• Storage: Dry, dark and at 2 - 8 °C for six months or -20°C for two years.
• IC50: 35 nM (CYP11B1), 0.7 nM (human aldosterone synthase), and 160 nM (rat aldosterone synthase)
• InChI: InChI=1S/C13H10FN3/c14-12-5-9(6-15)1-3-11(12)13-4-2-10-7-16-8-17(10)13/h1,3,5,7-8,13H,2,4H2/t13-/m1/s1
• InChIKey: USUZGMWDZDXMDG-CYBMUJFWSA-N
• SMILES: C1CC2=CN=CN2[C@H]1C3=C(C=C(C=C3)C#N)F

Osilodrostat（Cat No.:I008509）is an oral cortisol synthesis inhibitor used to treat Cushing’s disease in adults who are not candidates for surgery or have failed surgical intervention. It works by inhibiting the enzyme 11β-hydroxylase, which is crucial for cortisol production in the adrenal glands. By reducing excessive cortisol levels, Osilodrostat helps manage the symptoms of Cushing’s disease, such as weight gain, hypertension, and glucose intolerance. Its efficacy in lowering cortisol makes it a key option for controlling hypercortisolism, offering relief for patients with this challenging endocrine disorder.

Reference

[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.
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[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.
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[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.
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