Biological Activity
Cytochrome P450 inhibitor. Inhibits several cytochrome P450 enzymes including aromatase (CYP19) and retinoic acid 4-hydroxylase (CYP26). Blocks retinoic acid metabolism (retinoic acid metabolism blocking agent, RAMBA). Displays antitumor activity against androgen-dependent and independent rat prostate carcinomas.
Compound Libraries
Liarozole dihydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 381.69 |
| Formula | C17H13ClN4.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| PubChem ID | 121513844 |
| InChI Key | NKDMRTVUEJWCCQ-UHFFFAOYSA-N |
| Smiles | ClC1=CC(C(N4C=CN=C4)C2=CC=C(N=CN3)C3=C2)=CC=C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.17 | 100 | |
| water | 34.52 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 381.69. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.62 mL | 13.1 mL | 26.2 mL |
| 5 mM | 0.52 mL | 2.62 mL | 5.24 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.62 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Van Wauwe et al (1992) Liarozole, an inhibitor of retinoic acid metabolism, exerts retinoid-mimetic effects in vivo. J.Pharmacol.Exp.Ther. 261 773 PMID: 1374473
Njar et al (2006) Retinoic acid metabolism blocking agents (RAMBAs) for treatment of cancer and dermatological diseases. Bioorg.Med.Chem. 14 4323 PMID: 16530416
Goss et al (2007) Effects of liarozole fumarate (R85246) in combination with tamoxifen on N-methyl-N-nitrosourea (MNU)-induced mammary carcinoma and uterus in the rat model. BMC Cancer 7 26 PMID: 17266767
Keywords: Liarozole dihydrochloride, supplier, Cytochrome, P450, CYP26, inhibitors, inhibits, blocks, retinoic, acid, metabolism, Blocks, RXR, Retinoid, X, Receptors, CYP, RAR, RAMBA, Retinoic, Acid, R75251, R-75251, Retinoic, Acid, Receptors, Cytochrome, P450, Retinoid, X, Receptor, Retinoic, Acid, Receptors, Tocris Bioscience
