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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C13H10FN3 |
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分子量 | 227.24 | CAS No. | 928134-65-0 | |
Solubility (25°C)* | 体外 | DMSO | 45 mg/mL (198.02 mM) | |
Ethanol | 45 mg/mL (198.02 mM) | |||
Water | Insoluble | |||
* <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. |
製品説明 | LCI699 (Osilodrostat) is a potent inhibitor of 11β-hydroxylase (CYP11B), an enzyme catalyzing the final step of cortisol synthesis. |
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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]. |
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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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。