Liarozole dihydrochloride

Pricing Availability   Qty
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 (3)
Reviews
Literature (1)

Biological Activity for Liarozole dihydrochloride

Liarozole 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.

Compound Libraries for Liarozole dihydrochloride

Liarozole dihydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Liarozole dihydrochloride

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.

Solubility Data for Liarozole dihydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 38.17 100
water 34.52 100

Preparing Stock Solutions for Liarozole dihydrochloride

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.

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 for Liarozole dihydrochloride

Certificate of Analysis / Product Datasheet
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References for Liarozole dihydrochloride

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

3 Citations for Liarozole dihydrochloride

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


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Retinoid Receptors Scientific Review

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.