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Technical Data
| Formula | C13H10FN3 |
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| Molecular Weight | 227.24 | CAS No. | 928134-65-0 | |
| 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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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | LCI699(Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis. | ||
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| Targets |
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| In vitro | LCI699 also inhibits aldosterone synthase (CYP11B2) other than CYP11B1[1]. | ||
| 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[1]. The administration of LCI699, up to 1.0 mg BID, effectively and safely inhibits aldosterone synthase in patients with primary aldosteronism[2]. |
Protocol (from reference)
References
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Selleck's Osilodrostat (LCI699) has been cited by 4 publications
| Development of Human Pituitary Neuroendocrine Tumor Organoids to Facilitate Effective Targeted Treatments of Cushing's Disease [ Cells, 2022, 11(21)3344] | PubMed: 36359740 |
| Predictive In Vitro-In Vivo Extrapolation for Time Dependent Inhibition of CYP1A2, CYP2C8, CYP2C9, CYP2C19, and CYP2D6 Using Pooled Human Hepatocytes, Human Liver Microsomes, and a Simple Mechanistic Static Model [ Drug Metab Dispos, 2022, 50(2):114-127] | PubMed: 34789487 |
| Redox partner adrenodoxin alters cytochrome P450 11B1 ligand binding and inhibition [ J Inorg Biochem, 2022, 235:111934] | PubMed: 35952394 |
| Structural and functional insights into aldosterone synthase interaction with its redox partner protein adrenodoxin [ J Biol Chem, 2021, S0021-9258(21)00587-1] | PubMed: 34015331 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.