Home>>Lipids>> P450>>Liarozole dihydrochloride

Liarozole dihydrochloride (Synonyms: R75251 dihydrochloride)

Catalog No.GC38554

?Liarozole dihydrochloride is a P-450 inhibitor and retinoic acid (RA) metabolizing blocking agent inhibits RA metabolism and thereby increases intracellular RA levels in cells that actively produce RA.

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Liarozole dihydrochloride Chemical Structure

Cas No.: 1883548-96-6

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25mg
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50mg
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100mg
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200mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

Hepatocellular carcinoma cell line (Huh-7)

Preparation Method

Huh-7 cells were treated with Liarozole for 72 hours, followed by subjecting cell lysates to immunoblotting with Pin1 antibody.

Reaction Conditions

1,5,10,25,50 µM Liarozole for 72 h.

Applications

Liarozole combination with ATRA potently increased the ability of ATRA to induce proline isomerase (Pin1) degradation.Pin1 knockdown suppresses cell proliferation in various human HCC cell lines.

Animal experiment [2]:

Animal models

Sprague-Dawley rats

Preparation Method

Sprague Dawley rats were ovariectomized (OVX) 7 days before the start of the experiment. At 21 days of age the animals were weighed and randomized to treatment groups. Liarozole and vehicle hydroxypropyl-β- cyclodextrin were given twice daily by oral gavage.

Dosage form

20, 80mg/kg Liarozole, oral gavages

Applications

The cumulative tumor growth was significantly slower in Liarozole treatment groups compared to the control group.Liarozole was only able to stop tumor growth. When given in combination, liarozole (80 mg/kg) plus tamoxifen (100 mg/kg) was more effective than liarozole alone.

References:

[1]. Liao XH, Zhang AL, et al.Chemical or genetic Pin1 inhibition exerts potent anticancer activity against hepatocellular carcinoma by blocking multiple cancer-driving pathways. Sci Rep. 2017 Mar 6;7:43639.

[2]. Goss PE, Strasser-Weippl K, et al.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. 2007 Jan 31;7:26.

Background

Liarozole dihydrochloride is a P-450 inhibitor and retinoic acid (RA) metabolizing blocking agent inhibits RA metabolism and thereby increases intracellular RA levels in cells that actively produce RA. Liarozole has been used in the treatment of a variety of conditions characterized by extracellular matrix (ECM) overproduction such as ichthyosis[1].

IC50 values for P-450 Inhibitors Liarozole was determined as 4.2 µM, using male rat hepatic microsomes and 3uM retinoic acid as substrate[2]. Liarozole combination with ATRA potently increased the ability of ATRA to induce proline isomerase (Pin1) degradation.Pin1 knockdown suppresses cell proliferation in various human HCC cell lines. When the concentration of ATRA was fixed at 10 μM, Pin1 was degraded in a dose dependent manner depending on increasing concentrations of liarozole, with IC50 ~24.5 μM[3]

The cumulative tumor growth was significantly slower in Liarozole compared to the control group (p = 0.0001). Both liarozole and tamoxifen when given alone demonstrated anti-tumor effects. However, while tamoxifen lead to tumor shrinkage, liarozole was only able to stop tumor growth. When given in combination, liarozole (80 mg/kg) plus tamoxifen (100 mg/kg) was more effective than liarozole alone (p = 0.0001). There were no significant differences between the two doses of liarozole either when given alone (p = 0.49) or in combination with tamoxifen (p = 0.8)[4]

References:
[1]. Levy G, Malik M, et al. Liarozole inhibits transforming growth factor-β3--mediated extracellular matrix formation in human three-dimensional leiomyoma cultures. Fertil Steril. 2014 Jul;102(1):272-281.e2.
[2]. Ahmad M. Study on cytochrome p-450 dependent retinoic Acid metabolism and its inhibitors as potential agents for cancer therapy. Sci Pharm. 2011 Oct-Dec;79(4):921-35.
[3]. Liao XH, Zhang AL, et al.Chemical or genetic Pin1 inhibition exerts potent anticancer activity against hepatocellular carcinoma by blocking multiple cancer-driving pathways. Sci Rep. 2017 Mar 6;7:43639.
[4]. Goss PE, Strasser-Weippl K, et al.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. 2007 Jan 31;7:26.

Chemical Properties

Cas No. 1883548-96-6 SDF
Synonyms R75251 dihydrochloride
Canonical SMILES ClC1=CC(C(C2=CC=C3N=CNC3=C2)N4C=CN=C4)=CC=C1.[H]Cl.[H]Cl
Formula C17H15Cl3N4 M.Wt 381.69
Solubility Water: ≥ 50 mg/mL (131.00 mM); DMSO: 50 mg/mL (131.00 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6199 mL 13.0996 mL 26.1993 mL
5 mM 0.524 mL 2.6199 mL 5.2399 mL
10 mM 0.262 mL 1.31 mL 2.6199 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 28 reference(s) in Google Scholar.)

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