Osilodrostat free base

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MedKoo CAT#: 205909

CAS#: 928134-65-0 (free base)

Description: Osilodrostat, also known as LCI699, is a potent inhibitor of 11β-hydroxylase, the enzyme which catalyzes the final step of cortisol synthesis. LCI699 may thus be a potential new treatment for all forms of Cushing's syndrome. Current evidence indicates that the novel aldosterone inhibitor LCI699 is an effective and well-tolerated antihypertensive agent that lowers plasma aldosterone concentration and produces a mild ACTH-stimulated cortisol response suppressive effect.

Chemical Structure

Osilodrostat free base
CAS# 928134-65-0 (free base)

Theoretical Analysis

MedKoo Cat#: 205909
Name: Osilodrostat free base
CAS#: 928134-65-0 (free base)
Chemical Formula: C13H10FN3
Exact Mass: 227.08588
Molecular Weight: 227.237
Elemental Analysis: C, 68.71; H, 4.44; F, 8.36; N, 18.49

Price and Availability

Size Price Availability Quantity
5.0mg USD 150.0 Ready to ship
10.0mg USD 250.0 Ready to ship
25.0mg USD 450.0 Ready to ship
50.0mg USD 750.0 Ready to ship
100.0mg USD 1350.0 Ready to ship
200.0mg USD 2350.0 Ready to ship
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Related CAS #: 928134-65-0 (free base)   928134-31-0 (free base)   1315449-72-9 (phosphate)  

Synonym: LCI699; LCI 699; LCI-699; Osilodrostat; Osilodrostat free base

IUPAC/Chemical Name: (R)-4-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)-3-fluorobenzonitrile


InChi Code: 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

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

Appearance: Solid powder

Purity: >98%

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >5 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 227.237 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Guelho D, Grossman AB. Emerging drugs for Cushing's disease. Expert Opin Emerg Drugs. 2015 Sep;20(3):463-78. doi: 10.1517/14728214.2015.1047762. Epub 2015 Jun 2. PubMed PMID: 26021183.

2: Li L, Vashisht K, Boisclair J, Li W, Lin TH, Schmid HA, Kluwe W, Schoenfeld H, Hoffmann P. 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. doi: 10.1016/j.taap.2015.05.004. Epub 2015 May 14. PubMed PMID: 25981165.

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5: Wang HZ, Tian JB, Yang KH. Efficacy and safety of LCI699 for hypertension: a meta-analysis of randomized controlled trials and systematic review. Eur Rev Med Pharmacol Sci. 2015;19(2):296-304. Review. PubMed PMID: 25683946.

6: Daniel E, Newell-Price JD. Therapy of endocrine disease: steroidogenesis enzyme inhibitors in Cushing's syndrome. Eur J Endocrinol. 2015 Jun;172(6):R263-80. doi: 10.1530/EJE-14-1014. Epub 2015 Jan 30. Review. PubMed PMID: 25637072.

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8: Ménard J, Rigel DF, Watson C, Jeng AY, Fu F, Beil M, Liu J, Chen W, Hu CW, Leung-Chu J, LaSala D, Liang G, Rebello S, Zhang Y, Dole WP. 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. doi: 10.1186/s12967-014-0340-9. PubMed PMID: 25491597; PubMed Central PMCID: PMC4301837.

9: Oki Y. Medical management of functioning pituitary adenoma: an update. Neurol Med Chir (Tokyo). 2014;54(12):958-65. Epub 2014 Nov 29. PubMed PMID: 25446388.

10: Cai TQ, Stribling S, Tong X, Xu L, Wisniewski T, Fontenot JA, Struthers M, Akinsanya KO. Rhesus monkey model for concurrent analyses of in vivo selectivity, pharmacokinetics and pharmacodynamics of aldosterone synthase inhibitors. J Pharmacol Toxicol Methods. 2015 Jan-Feb;71:137-46. doi: 10.1016/j.vascn.2014.09.011. Epub 2014 Oct 7. PubMed PMID: 25304940.

11: Lother A, Moser M, Bode C, Feldman RD, Hein L. Mineralocorticoids in the heart and vasculature: new insights for old hormones. Annu Rev Pharmacol Toxicol. 2015;55:289-312. doi: 10.1146/annurev-pharmtox-010814-124302. Epub 2014 Sep 10. Review. PubMed PMID: 25251996.

12: Cuevas-Ramos D, Fleseriu M. Treatment of Cushing's disease: a mechanistic update. J Endocrinol. 2014 Nov;223(2):R19-39. doi: 10.1530/JOE-14-0300. Epub 2014 Aug 18. Review. PubMed PMID: 25134660.

13: Yin L, Hu Q, Emmerich J, Lo MM, Metzger E, Ali A, Hartmann RW. Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors. J Med Chem. 2014 Jun 26;57(12):5179-89. doi: 10.1021/jm500140c. Epub 2014 Jun 5. PubMed PMID: 24899257.

14: Li W, Luo S, Rebello S, Flarakos J, Tse FL. A semi-automated LC-MS/MS method for the determination of LCI699, a steroid 11β-hydroxylase inhibitor, in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci. 2014 Jun 1;960:182-93. doi: 10.1016/j.jchromb.2014.04.012. Epub 2014 Apr 30. PubMed PMID: 24814004.

15: Trainer PJ. Next generation medical therapy for Cushing's syndrome--can we measure a benefit? J Clin Endocrinol Metab. 2014 Apr;99(4):1157-60. doi: 10.1210/jc.2014-1054. PubMed PMID: 24702012.

16: Bertagna X, Pivonello R, Fleseriu M, Zhang Y, Robinson P, Taylor A, Watson CE, Maldonado M, Hamrahian AH, Boscaro M, Biller BM. LCI699, a potent 11β-hydroxylase inhibitor, normalizes urinary cortisol in patients with Cushing's disease: results from a multicenter, proof-of-concept study. J Clin Endocrinol Metab. 2014 Apr;99(4):1375-83. doi: 10.1210/jc.2013-2117. Epub 2013 Dec 11. PubMed PMID: 24423285.

17: Oki Y. Medical management of functioning pituitary adenoma: an update. Neurol Med Chir (Tokyo). 2014;54 Suppl 3:958-65. PubMed PMID: 26236804.

18: Schumacher CD, Steele RE, Brunner HR. Aldosterone synthase inhibition for the treatment of hypertension and the derived mechanistic requirements for a new therapeutic strategy. J Hypertens. 2013 Oct;31(10):2085-93. doi: 10.1097/HJH.0b013e328363570c. PubMed PMID: 24107737; PubMed Central PMCID: PMC3771574.

19: Brown NJ. Contribution of aldosterone to cardiovascular and renal inflammation and fibrosis. Nat Rev Nephrol. 2013 Aug;9(8):459-69. doi: 10.1038/nrneph.2013.110. Epub 2013 Jun 18. Review. PubMed PMID: 23774812; PubMed Central PMCID: PMC3922409.

20: van der Pas R, de Herder WW, Hofland LJ, Feelders RA. Recent developments in drug therapy for Cushing's disease. Drugs. 2013 Jun;73(9):907-18. doi: 10.1007/s40265-013-0067-6. Review. PubMed PMID: 23737437.

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