| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally bioavailable, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase). Liarozole dihydrochloride prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid sparing and retinoid-mimetic effects in vivo. Liarozole dihydrochloride is an imidazole analogue; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.
| 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].
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| 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].
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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. |
| 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. |
| References |
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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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