LY 78335
Based on 1 Customer Validation
LY 78335 (DCMB) is a brain-penetrant phenylethanolamine-N-methyltransferase (PNMT) inhibitor with a Ki of 0.09 μM. LY 78335 acts as an α₂-adrenoceptor inhibitor with an IC50 of 10 μM. LY 78335 increases spontaneous locomotor activity in rats. LY 78335 increases extracellular concentration of 3-methoxy-4-hydroxyphenylglycol (MHPG) in rat hypothalamus. LY 78335 prevents growth hormone (GH) secretion in rats. LY 78335 can be used for the research of depression.
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: 99.19%
- CAS 番号: 39226-94-3
- 分子式: C8H9Cl2N
- 分子量:190.07
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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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Adrenergic Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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α2-adrenergic receptor 10 μM (IC50) |
PNMT 0.09 μM (Ki) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, 10-week-old, initially 8-week-old, fed for 2 weeks before experiments)[1]
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Dosage:50 mg/kg
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Administration:i.p.; single dose
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Result:Increased spontaneous locomotor activity; increased extracellular MHPG concentration in the hypothalamus; blocked clonidine-induced GH secretion.
化学情報
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CAS 番号 39226-94-3
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性状 Liquid
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分子量 190.07
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分子式 C8H9Cl2N
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Color Light yellow to yellow
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SMILES
ClC1=CC=CC(=C1Cl)C(N)C
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別名
DCMB
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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 (526.12 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 (13.15 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 (13.15 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
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 (274 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Fuller RW, et al. Inhibition of phenylethanolamine N-methyltransferase by benzylamines. 2. In vitro and in vivo studies with 2,3-dichloro-methylbenzylamine. J Med Chem. 1973 Feb;16(2):106-9. [Content Brief]
[2]. Kuboia M, et al. Effect of a phenylethanolamine N-methyltransferase inhibitor, 2,3-dichloro-alpha-methylbenzylamine, on the alpha-2-adrenoceptor function in the hypothalamus in rats. Neuropsychobiology. 1996;33(3):132-7. [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 | 5.2612 mL | 26.3061 mL | 52.6122 mL | 131.5305 mL |
| 5 mM | 1.0522 mL | 5.2612 mL | 10.5224 mL | 26.3061 mL | |
| 10 mM | 0.5261 mL | 2.6306 mL | 5.2612 mL | 13.1530 mL | |
| 15 mM | 0.3507 mL | 1.7537 mL | 3.5075 mL | 8.7687 mL | |
| 20 mM | 0.2631 mL | 1.3153 mL | 2.6306 mL | 6.5765 mL | |
| 25 mM | 0.2104 mL | 1.0522 mL | 2.1045 mL | 5.2612 mL | |
| 30 mM | 0.1754 mL | 0.8769 mL | 1.7537 mL | 4.3843 mL | |
| 40 mM | 0.1315 mL | 0.6577 mL | 1.3153 mL | 3.2883 mL | |
| 50 mM | 0.1052 mL | 0.5261 mL | 1.0522 mL | 2.6306 mL | |
| 60 mM | 0.0877 mL | 0.4384 mL | 0.8769 mL | 2.1922 mL | |
| 80 mM | 0.0658 mL | 0.3288 mL | 0.6577 mL | 1.6441 mL | |
| 100 mM | 0.0526 mL | 0.2631 mL | 0.5261 mL | 1.3153 mL |
LY 78335 関連分類
HY-142110 関連分類
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