Liarozole dihydrochloride

Pricing Availability Delivery Time Qty
Cat.No. 2705 - Liarozole dihydrochloride | C17H13ClN4.2HCl
Description: Blocks retinoic acid metabolism
Alternative Names: R-75251
Chemical Name: 5-[(3-Chlorophenyl)-1H-imidazol-1-ylmethyl]-1H-benzimidazole dihydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations (2)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


If you know of a relevant reference for Liarozole dihydrochloride, please let us know.

Keywords: 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

2 Citations for Liarozole dihydrochloride

Citations are publications that use Tocris products. Selected citations for Liarozole dihydrochloride include:

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? If so please let us know.

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Reviews

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
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  • Invasion and Metastasis
Nuclear Receptors

Nuclear Receptors Product Listing

A collection of over 150 products for key nuclear receptors, the listing includes research tools for the study of:

  • Androgen Receptors
  • Estrogen Receptors
  • Retinoic Acid Receptors
  • Retinoid X Receptors
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Retinoid Receptors

Retinoid Receptors Scientific Review

Written by Alexander Moise, this review summarizes the nature of retinoid receptors, their isotype and isoform variants and modulation of retinoid signaling. Compounds available from Tocris are listed.

Pathways for Liarozole dihydrochloride

Protocols

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