Roxindole hydrochloride
Based on 1 Customer Validation
Roxindole hydrochloride (EMD 38362), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor with high affinity for 5-HT1A (IC50=0.9 nM). Antipsychotic and antidepressant activities.
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 : 99.01%
- CAS 番号: 108050-82-4
- 分子式: C23H27ClN2O
- 分子量:382.93
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Dopamine 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
製品説明
IC50 & Target
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D2 Receptor |
5-HT1A Receptor |
体内実験
Roxindole hydrochloride (1, 3, 10 mg/kg; s.c) inhibits both effects of 8-OH-DPAT (flat body and forepaw treading) in normal rats (male Wistar 200-350g)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 108050-82-4
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性状 Solid
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分子量 382.93
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分子式 C23H27ClN2O
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Color White to off-white
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SMILES
OC1=CC2=C(C=C1)NC=C2CCCCN3CCC(C4=CC=CC=C4)=CC3.[H]Cl
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別名
EMD 38362
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
溶剤 & 溶解度
体外:
DMSO : 50 mg/mL (130.57 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 1 mg/mL (2.61 mM; ultrasonic and warming and heat to 60°C)
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, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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: ≥ 2.08 mg/mL (5.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.43 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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, stored under nitrogen)
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 (271 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Bartoszyk GD, Harting J, Minck KO. Roxindole: psychopharmacological profile of a dopamine D2 autoreceptor agonist. J Pharmacol Exp Ther. 1996;276(1):41-48. [Content Brief]
[2]. Wetzel H, et al. Roxindole, a dopamine autoreceptor agonist, in the treatment of positive and negative schizophrenic symptoms. Am J Psychiatry. 1994;151(10):1499-1502. [Content Brief]
[3]. Maj J, et al. Roxindole, a dopamine autoreceptor agonist with a potential antidepressant activity. II. Effects on the 5-hydroxytryptamine system. Pharmacopsychiatry. 1997;30(2):55-61. [Content Brief]
[4]. Prehn JH, et al. Effects of serotonergic drugs in experimental brain ischemia: evidence for a protective role of serotonin in cerebral ischemia. Brain Res. 1993;630(1-2):10-20. [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, stored under nitrogen). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.6114 mL | 13.0572 mL | 26.1144 mL | 65.2861 mL |
| DMSO | 5 mM | 0.5223 mL | 2.6114 mL | 5.2229 mL | 13.0572 mL |
| 10 mM | 0.2611 mL | 1.3057 mL | 2.6114 mL | 6.5286 mL | |
| 15 mM | 0.1741 mL | 0.8705 mL | 1.7410 mL | 4.3524 mL | |
| 20 mM | 0.1306 mL | 0.6529 mL | 1.3057 mL | 3.2643 mL | |
| 25 mM | 0.1045 mL | 0.5223 mL | 1.0446 mL | 2.6114 mL | |
| 30 mM | 0.0870 mL | 0.4352 mL | 0.8705 mL | 2.1762 mL | |
| 40 mM | 0.0653 mL | 0.3264 mL | 0.6529 mL | 1.6322 mL | |
| 50 mM | 0.0522 mL | 0.2611 mL | 0.5223 mL | 1.3057 mL | |
| 60 mM | 0.0435 mL | 0.2176 mL | 0.4352 mL | 1.0881 mL | |
| 80 mM | 0.0326 mL | 0.1632 mL | 0.3264 mL | 0.8161 mL | |
| 100 mM | 0.0261 mL | 0.1306 mL | 0.2611 mL | 0.6529 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.