| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg | |||
| Other Sizes |
| Targets |
Liarozole dihydrochloride targets cytochrome P450 enzymes, a family of heme-containing monooxygenases involved in the metabolism of drugs and endogenous compounds. As a cytochrome P450 inhibitor, Liarozole modulates the metabolism of retinoids and other substrates, leading to altered signaling pathways involved in cell proliferation and differentiation. The compound displays antitumor activity against androgen-dependent and independent rat prostate carcinomas. Its mechanism of action involves the inhibition of retinoid metabolism, resulting in increased retinoid levels and subsequent antitumor effects.
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| ln Vitro |
Cell proliferation is inhibited by rizazole dihydrochloride (0.01~10 μM; 9 days; MCF-7 cells) [3]. Chondrogenesis in mesenchymal cells is totally inhibited by liarozole diHClide (1 μM; 4 days) [4].
In vitro, Liarozole dihydrochloride displays antitumor activity against prostate carcinoma cell lines. The compound's activity has been demonstrated in both androgen-dependent and independent models. As a cytochrome P450 inhibitor, Liarozole modulates the metabolism of retinoids and other substrates, leading to altered signaling pathways involved in cell proliferation and differentiation. The compound's in vitro activity has been characterized in various cancer cell lines. |
| ln Vivo |
Estrogen-stimulated vaginal keratosis is reversed with liarozole diHClide (5–20 mg/kg; oral) [5]. The oral dosage of 40 mg/kg of riazole dihydrochloride considerably lowers the tumor burden [6].
In vivo, Liarozole dihydrochloride has been studied in animal models of prostate cancer and other cancers. The compound displays antitumor activity against androgen-dependent and independent rat prostate carcinomas. Liarozole has been investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders. The compound has also been studied in dermatological conditions like psoriasis and ichthyosis. Further clinical studies are needed to fully characterize its therapeutic potential. |
| Enzyme Assay |
Liarozole dihydrochloride is not typically used in standard receptor binding assays. Its activity is assessed through cytochrome P450 enzyme inhibition assays or cell-based assays measuring antitumor activity. In enzyme inhibition assays, cytochrome P450 activity is measured by monitoring the metabolism of specific substrates. Liarozole dihydrochloride is incubated with the enzyme and substrate at varying concentrations, and product formation is quantified by HPLC or LC-MS. IC50 values are calculated from concentration-response curves.
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| Cell Assay |
Cell proliferation experiment [3]
Cell Types: MCF-7 cell Tested Concentrations: 0.01~10 μM Incubation Duration: 9 days Experimental Results: 35% inhibitory effect on cell proliferation at 10 μM. Cell differentiation analysis[4] Cell Types: Mesenchymal cells Tested Concentrations: 1 μM Incubation Duration: 4 days Experimental Results: Complete inhibition of chondrogenesis. Cellular assays for Liarozole dihydrochloride are performed using prostate cancer cell lines or other cancer cell lines. Cells are cultured in appropriate media and treated with Liarozole dihydrochloride at varying concentrations for defined time periods. Cell viability and proliferation are assessed using standard assays such as MTT, CellTiter-Glo, or colony formation assays. Apoptosis is assessed by measuring caspase activation, PARP cleavage, or Annexin V staining. The compound's effects on retinoid signaling may be assessed by measuring the expression of retinoid-regulated genes. |
| Animal Protocol |
Animal/Disease Models: ovariectomized rats
Doses: 5~20 mg/kg Route of Administration: Po Experimental Results: Reverse vaginal keratinization induced by estrogen stimulation. Animal/Disease Models: SCID (severe combined immunodeficient) mouse Doses: 40 mg/kg Route of Administration: Po Experimental Results: Inhibition of tumor growth and survival. In vivo studies with Liarozole dihydrochloride are conducted in animal models of prostate cancer and other cancers. The compound is administered via appropriate routes (e.g., oral or intraperitoneal) at defined doses and schedules. Tumor growth is monitored by caliper measurements, and tumor volumes are calculated. Tumor tissues are collected for histological analysis and assessment of signaling pathway modulation. The compound's antitumor activity has been demonstrated in rat prostate carcinoma models. |
| ADME/Pharmacokinetics |
Liarozole dihydrochloride has a molecular weight of 381.69 and a molecular formula of C17H13ClN4 · 2HCl. The compound is soluble in water at 2 mg/mL. Detailed pharmacokinetic parameters, including oral bioavailability and half-life, have been characterized in preclinical and clinical studies. The compound has been investigated in cancer research, particularly prostate and breast cancer, as well as in dermatological conditions.
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| Toxicity/Toxicokinetics |
Liarozole dihydrochloride has been studied in preclinical and clinical settings for its safety and efficacy. The compound is intended for research use only and is not currently approved for human therapeutic applications. Common side effects associated with cytochrome P450 inhibitors may include gastrointestinal disturbances and skin reactions. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment. The compound has a purity of ≥98-99%.
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| References |
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| Additional Infomation |
Liarozole dihydrochloride is an imidazole derivative and a cytochrome P450 inhibitor that displays antitumor activity. It has been investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders. The compound displays antitumor activity against androgen-dependent and independent rat prostate carcinomas. Liarozole dihydrochloride has been studied in cancer research, particularly prostate and breast cancer, as well as in dermatological conditions like psoriasis and ichthyosis. It is for research purposes only.
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| Molecular Formula |
C17H15CL3N4
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| Molecular Weight |
381.6868
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| Exact Mass |
380.036
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| CAS # |
1883548-96-6
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| Related CAS # |
Liarozole;115575-11-6
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| PubChem CID |
121513844
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
380
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C([H])C([H])=C([H])C(=C1[H])C([H])(C1C([H])=C([H])C2=C(C=1[H])N([H])C([H])=N2)N1C([H])=NC([H])=C1[H].Cl[H].Cl[H]
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| InChi Key |
NKDMRTVUEJWCCQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H13ClN4.2ClH/c18-14-3-1-2-12(8-14)17(22-7-6-19-11-22)13-4-5-15-16(9-13)21-10-20-15;;/h1-11,17H,(H,20,21);2*1H
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| Chemical Name |
6-[(3-chlorophenyl)-imidazol-1-ylmethyl]-1H-benzimidazole;dihydrochloride
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| Synonyms |
R75251 dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ≥ 50 mg/mL (~131.00 mM)
DMSO : ~50 mg/mL (~131.00 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (261.99 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6199 mL | 13.0996 mL | 26.1993 mL | |
| 5 mM | 0.5240 mL | 2.6199 mL | 5.2399 mL | |
| 10 mM | 0.2620 mL | 1.3100 mL | 2.6199 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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