WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 561472
CAS#: 1315449-72-9 (phosphate)
Description: Osilodrostat phosphate is a potent oral 11β-hydroxylase inhibitor. It is being studied for possible use in treatment of Cushing's disease.
MedKoo Cat#: 561472
Name: Osilodrostat phosphate
CAS#: 1315449-72-9 (phosphate)
Chemical Formula: C13H13FN3O4P
Exact Mass: 227.0859
Molecular Weight: 325.2362
Elemental Analysis: C, 48.01; H, 4.03; F, 5.84; N, 12.92; O, 19.68; P, 9.52
This product is not in stock, which may be available by custom synthesis.
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Related CAS #: 928134-65-0 (free base) 928134-31-0 (free base) 1315449-72-9 (phosphate)
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
Appearance: Solid powder
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
The following data is based on the product molecular weight 325.2362 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.
3: Fleseriu M, Castinetti F. Updates on the role of adrenal steroidogenesis inhibitors in Cushing's syndrome: a focus on novel therapies. Pituitary. 2016 Dec;19(6):643-653. Review. PubMed PMID: 27600150; PubMed Central PMCID: PMC5080363.
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.
