| CAS NO: | 928134-65-0 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 227.24 |
|---|---|
| Formula | C13H10FN3 |
| CAS No. | 928134-65-0 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 45 mg/mL (198.0 mM) |
| Water: 15 mg/mL (66.0 mM) | |
| Ethanol: 45 mg/mL (198.0 mM) | |
| Solubility (In vivo) | Chemical Name: (R)-4-(6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)-3-fluorobenzonitrile InChi Key: USUZGMWDZDXMDG-CYBMUJFWSA-N InChi Code: 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 SMILES Code: N#CC1=CC=C([C@H]2CCC3=CN=CN32)C(F)=C1 |
| Synonyms | Osilodrostat; LCI699; Isturisa; LCI 699; LCI-699 |
| In Vitro | In vitro activity: 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. |
| Animal model | |
| Formulation & Dosage | |
| References | J Clin Endocrinol Metab. 2014 Apr;99(4):1375-83; Hypertension. 2010 Nov;56(5):831-8. |
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