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Submit ReviewLiarozole dihydrochloride is a 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.
Liarozole dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 381.69 |
Formula | C17H13ClN4.2HCl |
Storage | Desiccate at RT |
Purity | ≥99% (HPLC) |
CAS Number | 1883548-96-6 |
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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 38.17 | 100 | |
water | 34.52 | 100 |
The following data is based on the product molecular weight 381.69. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
References are publications that support the biological activity of the product.
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 tamox. on N-methyl-N-nitrosourea (MNU)-induced mammary carcinoma and uterus in the rat model. BMC Cancer 7 26 PMID: 17266767
If you know of a relevant reference for Liarozole dihydrochloride, please let us know.
Keywords: Liarozole dihydrochloride, 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, Receptor, 2705, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Liarozole dihydrochloride include:
Bunt et al (2016) Insights into islet development and biology through characterization of a human iPSC-derived endocrine pancreas model. Islets 8 83 PMID: 27246810
Bhattacharya et al (2016) Normalizing Microbiota-Induced Retinoic Acid Deficiency Stimulates Protective CD8+ T Cell- Mediated Immunity in Colorectal Cancer Immunity 45 1 PMID: 27590114
Thomas and Henry (2014) Retinoic acid regulation by CYP26 in vertebrate lens regeneration. Neuropsychopharmacology 386 291 PMID: 24384390
Do you know of a great paper that uses Liarozole dihydrochloride from Tocris? Please let us know.
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