| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
Cell growth in MCF-7 cells is inhibited by rizazole (0.01~10 μM; 9 days) [3]. Chondrogenesis in mesenchymal cells is totally inhibited by liarozole (1 μM; 4 days) [4].
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|---|---|
| ln Vivo |
Estrogen-stimulated vaginal keratosis is reversed by rizazone (5–20 mg/kg; oral; 3 days) [5]. The tumor burden is greatly reduced by rizazol (40 mg/kg; oral; 21 days) [6].
|
| 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. |
| Animal Protocol |
Animal/Disease Models: ovariectomized rats [5]
Doses: 5~20 mg/kg Route of Administration: Po; 3-day Experimental Results: Reverse vaginal keratinization caused by estrogen stimulation. Animal/Disease Models: SCID (severe combined immunodeficient) mouse [6] Doses: 40 mg/kg Route of Administration: Po; 21-day Experimental Results: Inhibition of tumor growth and survival. |
| References |
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| Additional Infomation |
Liarozole is a member of benzimidazoles.
Liarozole has been used in trials studying the treatment of Ichthyosis, Lamellar. Liarozole is an orally-active benzimidazole derivative with potential antineoplastic activity. As a retinoic acid metabolism blocking agent, liarozole inhibits cytochrome P450-dependent all-trans-retinoic acid (ATRA)-4-hydroxylase, resulting in an increase in endogenous ATRA production, inhibition of cell proliferation, and induction of cell differentiation. This agent also inhibits aromatase, the enzyme that catalyzes the final, rate-limiting step in estrogen biosynthesis. See also: Liarozole Hydrochloride (annotation moved to). |
| Molecular Formula |
C17H13N4CL.HCL
|
|---|---|
| Molecular Weight |
345.22586
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| Exact Mass |
308.083
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| CAS # |
115575-11-6
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| Related CAS # |
Liarozole dihydrochloride;1883548-96-6
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| PubChem CID |
60652
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| Appearance |
Off-white to light yellow solid powder
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| Density |
1.36g/cm3
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| Boiling Point |
578.2ºC at 760mmHg
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| Flash Point |
303.5ºC
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| Vapour Pressure |
9.2E-13mmHg at 25°C
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| LogP |
4.05
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| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
22
|
| Complexity |
380
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
UGFHIPBXIWJXNA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H13ClN4/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)
|
| Chemical Name |
6-[(3-chlorophenyl)-imidazol-1-ylmethyl]-1H-benzimidazole
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
DMSO : ~100 mg/mL (~323.88 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.10 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 25.0 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: ≥ 2.5 mg/mL (8.10 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 25.0 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: ≥ 2.5 mg/mL (8.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8966 mL | 14.4831 mL | 28.9662 mL | |
| 5 mM | 0.5793 mL | 2.8966 mL | 5.7932 mL | |
| 10 mM | 0.2897 mL | 1.4483 mL | 2.8966 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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