115575-11-6
115575-11-6 structure
- Name: Liarozole
- Chemical Name: Liarozole
- CAS Number: 115575-11-6
- Molecular Formula: C17H13ClN4
- Molecular Weight: 308.76500
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Cytochrome P450
- Create Date: 2018-07-19 18:01:47
- Modify Date: 2024-01-09 12:19:36
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Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties[1][2][3].
| Name | Liarozole |
|---|---|
| Synonyms | MFCD00864664 |
| Description | Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties[1][2][3]. |
|---|---|
| Related Catalog | |
| Target |
Cytochrome P450 (CYP26):7 μM (IC50) |
| In Vitro | Liarozole (0.01~10 μM; 9 days; MCF-7 cells) inhibits cells proliferation[3]. Liarozole (1 μM; 4 days; mesenchymal cells) completely inhibits chondrogenesis[4]. Cell Proliferation Assay[3] Cell Line: MCF-7 cells Concentration: 0.01~10 μM Incubation Time: 9 days Result: Had an effect of 35% inhibition at 10 μM on cell proliferation. Cell Differentiation Assay[4] Cell Line: Mesenchymal cells Concentration: 1 μM Incubation Time: 4 days Result: Completely inhibited chondrogenesis. |
| In Vivo | Liarozole (5-20 mg/kg; p.o.; 3 days) reverses the vaginal keratosis caused by estrogen stimulation[5]. Liarozole (40 mg/kg; p.o.; 21 days) reduces tumor burden substantially[6]. Animal Model: Ovariectomized rats Dosage: 5~20 mg/kg Administration: P.o.; 3 days Result: Reversed the vaginal keratosis caused by estrogen stimulation. Animal Model: SCID mice Dosage: 40 mg/kg Administration: P.o.; 21 days Result: Inhibited tumor growth and survival. |
| References |
| Density | 1.36g/cm3 |
|---|---|
| Boiling Point | 578.2ºC at 760mmHg |
| Molecular Formula | C17H13ClN4 |
| Molecular Weight | 308.76500 |
| Flash Point | 303.5ºC |
| Exact Mass | 308.08300 |
| PSA | 46.50000 |
| LogP | 4.05050 |
| Vapour Pressure | 9.2E-13mmHg at 25°C |