Liarozole
Based on 1 Customer Validation
Liarozole (R75251; R85246) is an imidazole derivative and orally active retinoic acid (RA) metabolism-blocking agent (RAMBA). Liarozole inhibits the cytochrome P450 (CYP26)-dependent 4-hydroxylation of retinoic acid (IC50=7 μM), resulting in increased tissue levels of retinoic acid. Liarozole shows antitumoral properties.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.96%
- CAS 番号: 115575-11-6
- 分子式: C17H13ClN4
- 分子量:308.76
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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CYP26 7 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| HL-60 | IC50 |
0.89 μM
Compound: Liarozole
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Inhibition of CYP26A1 in ATRA-induced human HL60 cell microsomes incubated for 30 mins in dark condition with NADPH and ATRA by HPLC method
Inhibition of CYP26A1 in ATRA-induced human HL60 cell microsomes incubated for 30 mins in dark condition with NADPH and ATRA by HPLC method
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[PMID: 26365710] |
| HL-60 | IC50 |
2.45 μM
Compound: Liarozole
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Inhibition of CYP26A1 in ATRA-induced human HL60 cell microsomes incubated for 30 mins using ATRA and NADPH by HPLC method
Inhibition of CYP26A1 in ATRA-induced human HL60 cell microsomes incubated for 30 mins using ATRA and NADPH by HPLC method
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[PMID: 25684424] |
| MCF7 | IC50 |
540 nM
Compound: Liarozole
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Inhibition of CYP26A1 in human MCF7 cell microsomes using [3H]ATRA after 1 hr by scintillation counting
Inhibition of CYP26A1 in human MCF7 cell microsomes using [3H]ATRA after 1 hr by scintillation counting
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[PMID: 21428449] |
| MCF7 | IC50 |
7 μM
Compound: liarozole
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Inhibition of CYP26A1 in human MCF7 cells assessed as all-trans retinoic acid metabolism
Inhibition of CYP26A1 in human MCF7 cells assessed as all-trans retinoic acid metabolism
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[PMID: 16279770] |
| MCF7 | IC50 |
7 μM
Compound: Liarozole
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Inhibition of CYP26A1 in human MCF7 cells
Inhibition of CYP26A1 in human MCF7 cells
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[PMID: 18722776] |
| Sf9 | IC50 |
0.018 μM
Compound: 1
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Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase
Inhibition of microsomal fraction of human CYP26B1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 5 mins by HPLC analysis in presence of rat P450 reductase
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[PMID: 26918322] |
| Sf9 | IC50 |
1.9 μM
Compound: 1
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Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase
Inhibition of microsomal fraction of human CYP26A1 expressed in Sf9 cells using 9-cis-RA as substrate preincubated for 5 mins followed by NADPH addition measured after 1 min by HPLC analysis in presence of rat P450 reductase
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[PMID: 26918322] |
| SH-SY5Y | IC50 |
2.3 nM
Compound: Liar
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Increase in CYP26A1 mRNA expression in human SH-SY5Y cells after 72 hrs by RT-PCR analysis in the presence of 0.1 uM all-trans-retinoic acid
Increase in CYP26A1 mRNA expression in human SH-SY5Y cells after 72 hrs by RT-PCR analysis in the presence of 0.1 uM all-trans-retinoic acid
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[PMID: 21838328] |
Liarozole (0.01~10 μM; 9 days; MCF-7 cells) inhibits cells proliferation[3].
Liarozole (1 μM; 4 days; mesenchymal cells) completely inhibits chondrogenesis[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:0.01~10 μM
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Incubation Time:9 days
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Result:Had an effect of 35% inhibition at 10 μM on cell proliferation.
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Cell Line:Mesenchymal cells
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Concentration:1 μM
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Incubation Time:4 days
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Result:Completely inhibited chondrogenesis.
化学情報
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CAS 番号 115575-11-6
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性状 Solid
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分子量 308.76
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分子式 C17H13ClN4
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Color Off-white to light yellow
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SMILES
ClC1=CC(C(C2=CC=C3N=CNC3=C2)N4C=CN=C4)=CC=C1
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別名
R75251
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 100 mg/mL (323.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.10 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.10 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kuijpers AL, et al. The effects of oral liarozole on epidermal proliferation and differentiation in severe plaque psoriasis are comparable with those of acitretin. Br J Dermatol. 1998;139(3):380-389. [Content Brief]
[2]. Lucker GP, et al. Oral treatment of ichthyosis by the cytochrome P-450 inhibitor liarozole. Br J Dermatol. 1997;136(1):71-75. [Content Brief]
[3]. Wouters W, et al. Effects of liarozole, a new antitumoral compound, on retinoic acid-induced inhibition of cell growth and on retinoic acid metabolism in MCF-7 human breast cancer cells. Cancer Res. 1992;52(10):2841-2846. [Content Brief]
[4]. Pignatello MA, et al. Liarozole markedly increases all trans-retinoic acid toxicity in mouse limb bud cell cultures: a model to explain the potency of the aromatic retinoid (E)-4-[2-(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthylenyl)-1-propenyl] benzo [Content Brief]
[5]. Van Wauwe J, et al. Liarozole, an inhibitor of retinoic acid metabolism, exerts retinoid-mimetic effects in vivo. J Pharmacol Exp Ther. 1992;261(2):773-779. [Content Brief]
[6]. Stearns ME, et al. Liarozole and 13-cis-retinoic acid anti-prostatic tumor activity [published correction appears in Cancer Res 1993 Dec 1;53(23):5831]. Cancer Res. 1993;53(13):3073-3077. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2388 mL | 16.1938 mL | 32.3876 mL | 80.9690 mL |
| 5 mM | 0.6478 mL | 3.2388 mL | 6.4775 mL | 16.1938 mL | |
| 10 mM | 0.3239 mL | 1.6194 mL | 3.2388 mL | 8.0969 mL | |
| 15 mM | 0.2159 mL | 1.0796 mL | 2.1592 mL | 5.3979 mL | |
| 20 mM | 0.1619 mL | 0.8097 mL | 1.6194 mL | 4.0485 mL | |
| 25 mM | 0.1296 mL | 0.6478 mL | 1.2955 mL | 3.2388 mL | |
| 30 mM | 0.1080 mL | 0.5398 mL | 1.0796 mL | 2.6990 mL | |
| 40 mM | 0.0810 mL | 0.4048 mL | 0.8097 mL | 2.0242 mL | |
| 50 mM | 0.0648 mL | 0.3239 mL | 0.6478 mL | 1.6194 mL | |
| 60 mM | 0.0540 mL | 0.2699 mL | 0.5398 mL | 1.3495 mL | |
| 80 mM | 0.0405 mL | 0.2024 mL | 0.4048 mL | 1.0121 mL | |
| 100 mM | 0.0324 mL | 0.1619 mL | 0.3239 mL | 0.8097 mL |
Liarozole 関連分類
HY-106019 関連分類
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