Zonampanel
Based on 1 Customer Validation
Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.
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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: 99.02%
- CAS 番号: 210245-80-0
- 分子式: C13H9N5O6
- 分子量:331.24
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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
- プロトコル
- 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
Zonampanel inhibits the human MRP4-mediated transport of [3H]oestradiol 17-D-glucuronide in a concentration-dependent manner. In contrast, Zonampanel (up to 1000 mM) does not inhibit the human MRP2- or BCRP-mediated transport of [3H]oestradiol 17-D-glucuronide or [3H]methotrexate[1]. Zonampanel inhibits the uptake of typical substrates by Oat1, Oat2, and Oat3 with inhibition constant (Ki) values of 7.02 to 10.4 μM. A time- and saturable concentration-dependent increase in [14C]Zonampanel uptake is observed in these cells [Km values: 13.4 to 53.6 μM][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 210245-80-0
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性状 Solid
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分子量 331.24
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分子式 C13H9N5O6
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Color Yellow to brown
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SMILES
O=C(N1CC(O)=O)C(NC(C1=C2)=CC([N+]([O-])=O)=C2N3C=CN=C3)=O
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別名
YM 872
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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, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
DMSO : 50 mg/mL (150.95 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and 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 (7.55 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 (7.55 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 (sealed storage, away from moisture and 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.
プロトコル
Seven-week-old male Sprague-Dawley rats are used at 8 weeks after acclimatization for at least 1 week. During acclimatization, the rats are kept in an air-conditioned room with temperature and humidity controlled at 22.9 to 23.3°C and 50 to 78%; the room is lit for 12 h 30 min from 7:30 AM to 8:00 PM. Rats are given free access to solid food and water until just before drug administration. YM 872 (15 mg/kg) is administered at a single bolus dose into the rat tail vein with or without probenecid (50 mg/kg) or cimetidine (40 mg/kg). At 5, 15, and 30 min and 1, 2, 3, 4, and 6 h after dosing, blood is sampled under ether anesthesia via the inferior vena cava using a heparinized syringe and immediately stored on ice using four rats each per sampling time point per administration group (total of 128 rats for 8 sampling time points and 4 administration groups). Plasma is obtained by centrifugation at 4°C, 1870 g for 15 min and kept frozen at -20°C. Rats for plasma sampling at 3 and 6 h after administration are housed in metabolic cages after administration, spontaneously excreted urine is collected, and the cages are washed using water. Regarding specific gravity as 1, urine volume (including the cage-wash water) is calculated according to differences in the weight of the sampling tube before and after sampling. Urine samples are kept frozen at -20°C until assay as described below. All plasma and urine samples are protected from light throughout the sampling, storage, and assay procedures.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
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- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Minematsu T, et al. Characterization of renal tubular apical efflux of zonampanel, an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonist, in humans. Xenobiotica. 2008 Sep;38(9):1191-202. [Content Brief]
[2]. Minematsu T, et al. Role of organic anion transporters in the pharmacokinetics of zonampanel, an alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate receptor antagonist, in rats. Drug Metab Dispos. 2008 Aug;36(8):1496-504. [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 (sealed storage, away from moisture and 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 | 3.0190 mL | 15.0948 mL | 30.1896 mL | 75.4740 mL |
| 5 mM | 0.6038 mL | 3.0190 mL | 6.0379 mL | 15.0948 mL | |
| 10 mM | 0.3019 mL | 1.5095 mL | 3.0190 mL | 7.5474 mL | |
| 15 mM | 0.2013 mL | 1.0063 mL | 2.0126 mL | 5.0316 mL | |
| 20 mM | 0.1509 mL | 0.7547 mL | 1.5095 mL | 3.7737 mL | |
| 25 mM | 0.1208 mL | 0.6038 mL | 1.2076 mL | 3.0190 mL | |
| 30 mM | 0.1006 mL | 0.5032 mL | 1.0063 mL | 2.5158 mL | |
| 40 mM | 0.0755 mL | 0.3774 mL | 0.7547 mL | 1.8868 mL | |
| 50 mM | 0.0604 mL | 0.3019 mL | 0.6038 mL | 1.5095 mL | |
| 60 mM | 0.0503 mL | 0.2516 mL | 0.5032 mL | 1.2579 mL | |
| 80 mM | 0.0377 mL | 0.1887 mL | 0.3774 mL | 0.9434 mL | |
| 100 mM | 0.0302 mL | 0.1509 mL | 0.3019 mL | 0.7547 mL |
Zonampanel 関連分類
HY-15072 関連分類
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