Osavampator
Based on 1 Customer Validation
Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders.
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: 99.74%
- CAS 番号: 1358751-06-0
- 分子式: C19H23N3O3S
- 分子量:373.47
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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
- 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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iGluR 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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AMPA Receptor |
5-LO |
Osavampator (0.3 mg/kg, p.o., single dose) enhances sustained attention in the poor performing rats[2].
Osavampator (0.06 mg/kg, p.o., single dose) improves working memory in monkeys[2].
Osavampator (1 mg/kg, p.o., single dose) produces antidepressant-like effects in the rat RSBM (reduction of submissive behavior model)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Normal rats[2]
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Dosage:0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Improved the novelty discrimination index (NDI).
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Animal Model:Poor performing rats[2]
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Dosage:0.3 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Increased correct responses and decreased omissions in the poor performing rats.
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Animal Model:Fasted monkey[2]
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Dosage:0.06 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Significantly increased delayed match-to-sample (DMTS) accuracy at a 16-s delay interval. Maintained the beneficial effect 24 h after administration.
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Animal Model:submissive behavior model [1]
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Dosage:0.1 mg/kg, 1 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Led to a significant reduction in dominance levels compared with vehicle treatment starting from the seventh day of treatment and maintained throughout the study period. Had a significant effect in reducing dominance levels at 0.1 and 1 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1358751-06-0
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性状 Solid
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分子量 373.47
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分子式 C19H23N3O3S
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Color White to yellow
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SMILES
O=S1(N=C2C(C3=CC=C(C=C3)OC4CCCCC4)=NC(C)=CN2CC1)=O
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別名
TAK-653; NBI-1065845
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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 : ≥ 12.5 mg/mL (33.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 0.83 mg/mL (2.22 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 1 mg/mL (2.68 mM); Suspended solution; Need ultrasonic
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 (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Hara H, et al. TAK-653, an AMPA receptor potentiator with minimal agonistic activity, produces an antidepressant-like effect with a favorable safety profile in rats [J]. Pharmacology Biochemistry and Behavior, 2021, 211: 173289. [Content Brief]
[2]. Suzuki A, et al. Strictly regulated agonist-dependent activation of AMPA-R is the key characteristic of TAK-653 for robust synaptic responses and cognitive improvement [J]. Scientific Reports, 2021, 11(1): 14532. [Content Brief]
[3]. Hara H, et al. TAK-653, an AMPA receptor potentiator with minimal agonistic activity, produces an antidepressant-like effect with a favorable safety profile in rats. Pharmacol Biochem Behav. 2021 Dec;211:173289. [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 | 2.6776 mL | 13.3880 mL | 26.7759 mL | 66.9398 mL |
| 5 mM | 0.5355 mL | 2.6776 mL | 5.3552 mL | 13.3880 mL | |
| 10 mM | 0.2678 mL | 1.3388 mL | 2.6776 mL | 6.6940 mL | |
| 15 mM | 0.1785 mL | 0.8925 mL | 1.7851 mL | 4.4627 mL | |
| 20 mM | 0.1339 mL | 0.6694 mL | 1.3388 mL | 3.3470 mL | |
| 25 mM | 0.1071 mL | 0.5355 mL | 1.0710 mL | 2.6776 mL | |
| 30 mM | 0.0893 mL | 0.4463 mL | 0.8925 mL | 2.2313 mL |
Osavampator 関連分類
HY-115864 関連分類
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