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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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O413758-2mg | 2mg | In stock | $75.90 | |
O413758-5mg | 5mg | In stock | $107.90 | |
O413758-10mg | 10mg | In stock | $162.90 | |
O413758-25mg | 25mg | In stock | $271.90 | |
O413758-50mg | 50mg | In stock | $532.90 | |
O413758-100mg | 100mg | In stock | $924.90 |
P450(e.g. CYP17) Inhibitors
Synonyms | (R)-4-(6,7-Dihydro-5H-pyrrolo(1,2-c)imidazol-5-yl)-3-fluorobenzonitrile | GTPL8310 | 5YL4IQ1078 | OSILODROSTAT [WHO-DD] | Osilodrostat free base | Osilodrostat;4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile | TRICLOCARBAN (USP MO |
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Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of CYP11B1;Inhibitor of CYP11B2 |
Product Description | Information Osilodrostat (LCI699) LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B) , an enzyme catalyzing the final step of cortisol synthesis. Targets 11β-hydroxylase 2.5 nM In vitro LCI699 also inhibits aldosterone synthase (CYP11B2) other than CYP11B1. In vivo LCI699 is a potent inhibitor of 11β-hydroxylase (CYP11B1), the enzyme that catalyzes the final step of cortisol synthesis, and has a half-life of ∼4 hours. It decreases blood pressure (BP) in patients with essential hypertension and primary aldosteronism. Treatment with LCI699 is well tolerated, it is demonstrated efficacy with a satisfactory safety and tolerability profile in the proof-of-concept study in Cushing\'s disease. The administration of LCI699, up to 1.0 mg BID, effectively and safely inhibits aldosterone synthase in patients with primary aldosteronism. |
ALogP | 2.02 |
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Rotatable Bond | 1 |
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Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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IUPAC Name | 4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile |
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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 |
InChi Key | USUZGMWDZDXMDG-CYBMUJFWSA-N |
Canonical SMILES | C1CC2=CN=CN2C1C3=C(C=C(C=C3)C#N)F |
Isomeric SMILES | C1CC2=CN=CN2[C@H]1C3=C(C=C(C=C3)C#N)F |
PubChem CID | 44139752 |
Molecular Weight | 227.24 |
PubChem CID | 44139752 |
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ChEMBL Ligand | CHEMBL3099695 |
CAS Registry No. | 928134-65-0 |
RCSB PDB Ligand | YSY |
DrugCentral Ligand | 5384 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
---|---|---|---|
K2228505 | Certificate of Analysis | Sep 26, 2022 | O413758 |
K2228506 | Certificate of Analysis | Sep 26, 2022 | O413758 |
K2228507 | Certificate of Analysis | Sep 26, 2022 | O413758 |
K2228508 | Certificate of Analysis | Sep 26, 2022 | O413758 |
K2228509 | Certificate of Analysis | Sep 26, 2022 | O413758 |
K2228710 | Certificate of Analysis | Sep 26, 2022 | O413758 |
Solubility | Solubility (25°C) In vitro DMSO: 45 mg/mL (198.02 mM); Ethanol: 45 mg/mL (198.02 mM); Water: Insoluble; |
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DMSO(mg / mL) Max Solubility | 45 |
DMSO(mM) Max Solubility | 198.0285161 |
Water(mg / mL) Max Solubility | 15 |
Water(mM) Max Solubility | 66.00950537 |
Pictogram(s) | GHS07 |
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Signal | Warning |
Hazard Statements | H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H302:Harmful if swallowed |
Precautionary Statements | P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. |
1. Amar L, Azizi M, Menard J, Peyrard S, Watson C, Plouin PF. (2010) Aldosterone synthase inhibition with LCI699: a proof-of-concept study in patients with primary aldosteronism.. Hypertension, 56 (5): (831-8). [PMID:20837883] [10.1021/op500134e] |
2. Calhoun DA, White WB, Krum H, Guo W, Bermann G, Trapani A, Lefkowitz MP, Ménard J. (2011) Effects of a novel aldosterone synthase inhibitor for treatment of primary hypertension: results of a randomized, double-blind, placebo- and active-controlled phase 2 trial.. Circulation, 124 (18): (1945-55). [PMID:21986283] [10.1021/op500134e] |
3. Yin L, Hu Q, Emmerich J, Lo MM, Metzger E, Ali A, Hartmann RW. (2014) Novel pyridyl- or isoquinolinyl-substituted indolines and indoles as potent and selective aldosterone synthase inhibitors.. J Med Chem, 57 (12): (5179-89). [PMID:24899257] [10.1021/op500134e] |
4. Fleseriu M, Petersenn S. (2015) Medical therapy for Cushing's disease: adrenal steroidogenesis inhibitors and glucocorticoid receptor blockers.. Pituitary, 18 (2): (245-52). [PMID:25560275] [10.1021/op500134e] |
5. Daniel E, Newell-Price JD. (2015) Therapy of endocrine disease: steroidogenesis enzyme inhibitors in Cushing's syndrome.. Eur J Endocrinol, 172 (6): (R263-80). [PMID:25637072] [10.1021/op500134e] |
6. Wang HZ, Tian JB, Yang KH. (2015) Efficacy and safety of LCI699 for hypertension: a meta-analysis of randomized controlled trials and systematic review.. Eur Rev Med Pharmacol Sci, 19 (2): (296-304). [PMID:25683946] [10.1021/op500134e] |
7. Fleseriu M. (2015) Medical Treatment of Cushing Disease: New Targets, New Hope.. Endocrinol Metab Clin North Am, 44 (1): (51-70). [PMID:25732642] [10.1021/op500134e] |
8. Duggan S. (2020) Osilodrostat: First Approval.. Drugs, 80 (5): (495-500). [PMID:32141023] [10.1021/op500134e] |