Synonym
Osilodrostat phosphate; LCI699 phosphate; LCI-699 phosphate; LCI 699 phosphate;
IUPAC/Chemical Name
(R)-4-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)-3-fluorobenzonitrile phosphate
InChi Key
FMCPYRDGUZBOJZ-BTQNPOSSSA-N
InChi Code
InChI=1S/C13H10FN3.H3O4P/c14-12-5-9(6-15)1-3-11(12)13-4-2-10-7-16-8-17(10)13;1-5(2,3)4/h1,3,5,7-8,13H,2,4H2;(H3,1,2,3,4)/t13-;/m1./s1
SMILES Code
N#CC1=CC=C([C@H]2CCC3=CN=CN32)C(F)=C1.O=P(O)(O)O
Purity
>98% (or refer to the Certificate of Analysis)
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
Shelf Life
>2 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
325.24
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.
| 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 |
1: Cuevas-Ramos D, Lim DST, Fleseriu M. Update on medical treatment for Cushing's disease. Clin Diabetes Endocrinol. 2016 Sep 13;2:16. doi: 10.1186/s40842-016-0033-9. eCollection 2016. Review. PubMed PMID: 28702250; PubMed Central PMCID: PMC5471955.
2: Armani S, Ting L, Sauter N, Darstein C, Tripathi AP, Wang L, Zhu B, Gu H, Chun DY, Einolf HJ, Kulkarni S. Drug Interaction Potential of Osilodrostat (LCI699) Based on Its Effect on the Pharmacokinetics of Probe Drugs of Cytochrome P450 Enzymes in Healthy Adults. Clin Drug Investig. 2017 May;37(5):465-472. doi: 10.1007/s40261-017-0497-0. PubMed PMID: 28155129; PubMed Central PMCID: PMC5394143.
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4: Fleseriu M, Pivonello R, Young J, Hamrahian AH, Molitch ME, Shimizu C, Tanaka T, Shimatsu A, White T, Hilliard A, Tian C, Sauter N, Biller BM, Bertagna X. Osilodrostat, a potent oral 11β-hydroxylase inhibitor: 22-week, prospective, Phase II study in Cushing's disease. Pituitary. 2016 Apr;19(2):138-48. doi: 10.1007/s11102-015-0692-z. PubMed PMID: 26542280; PubMed Central PMCID: PMC4799251.
5: 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.
