| Identification | Back Directory | [Name]
LCI699 | [CAS]
928134-65-0 | [Synonyms]
LCI699
CS-2488
LCI 699NX
Osilodrostat
Osilodrostat (LCI699)
Isturisa (Osilodrostat)
Osilodrostat(LCI699) free base
4-(R)-(6,7-Dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl)-3-fluorobenzonitrile
4-[(5R)-6,7-Dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile
Benzonitrile, 4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluoro- | [Molecular Formula]
C13H10FN3 | [MDL Number]
MFCD25976825 | [MOL File]
928134-65-0.mol | [Molecular Weight]
227.24 |
| Chemical Properties | Back Directory | [Boiling point ]
433.8±45.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [solubility ]
DMSO:147.5(Max Conc. mg/mL);649.1(Max Conc. mM)
Ethanol:72.5(Max Conc. mg/mL);319.05(Max Conc. mM) | [form ]
A solid | [pka]
6.97±0.40(Predicted) | [color ]
White to yellow | [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 | [InChIKey]
USUZGMWDZDXMDG-CYBMUJFWSA-N | [SMILES]
C(#N)C1=CC=C([C@@H]2N3C(CC2)=CN=C3)C(F)=C1 |
| Hazard Information | Back Directory | [Uses]
Osilodrostat is a novel 11-β-hydroxylase inhibitor which may be used in the treatment of Cushing’s syndrome, | [in vivo]
Osilodrostat (LCI699; 0.1-100 mg/kg; p.o.; once) inhibits aldosterone and corticosterone synthesis in Ang-II- and ACTH-stimulated Sprague Dawley rats[1].
Osilodrostat (LCI699; 3-100 mg/kg; p.o.; daily, for 52 weeks) reduces mean arterial pressure and prolongs survival in dTG rats[1]. | Animal Model: | Male Ang-II- and ACTH-stimulated Sprague Dawley rats[1] | | Dosage: | 0.1, 0.3, 1 and 3 mg/kg (Ang-II-stimulated rats) and 1, 3, 10, 30 and 100 mg/kg (ACTH-stimulated rats) | | Administration: | Oral administration; once | | Result: | Inhibited the increase in plasma aldosterone concentrations stimulated by Ang II or ACTH in a dose-dependent manner. |
| Animal Model: | dTG rats[1] | | Dosage: | 3, 10, 30 and 100 mg/kg | | Administration: | Oral administration; daily, for 52 weeks | | Result: | Increased fractional LV (systolic and diastolic) shortening, normalized LV isovolumic relaxation time to RR (IVRT/RR) ratio and myocardial cell size and reduced LV weight in a dose-dependent manner. |
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