FR194921
Based on 1 Customer Validation
FR194921 is a potent, selective and orally active and cross the blood-brain barrier Adenosine A1 antagonist with Ki value of 6.6, 5400 nM for A1, A2A, respectively. FR194921 shows cognitive-enhancing and anxiolytic activity.
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: 98.54%
- CAS 番号: 202646-80-8
- 分子式: C23H23N5O
- 分子量:385.46
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Adenosine 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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A1R 6.6 nM (Ki) |
A2AR 5400 nM (Ki) |
FR194921 (0.032, 0.1, 0.32 mg/kg; p.o.) dose-dependently attenuates the hypolocomotion induced by CPA (HY-103181)[2].
FR194921 (0.1-10 mg/kg; i.p.) significantly ameliorates scopolamine (HY-N0296)-induced memory deficits[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SD rats[2]
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Dosage:0.032, 0.1, 0.32 mg/kg
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Administration:P.o.; administered orally 25 min prior to intraperitoneal administration of CPA (0.056 mg/kg; i.p.)
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Result:Dose-dependently attenuated the hypolocomotion induced by CPA with an ED50 value of 0.08 mg/kg and statistical significance at 0.32 mg/kg.
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Animal Model:SD rats[2]
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Dosage:0.1, 0.32, 1, 3.2, 10 mg/kg
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Administration:I.p.; Scopolamine (HY-N0296)(1 mg/kg, i.p.)
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Result:Significant cognitive enhanced following scopolamine-induced memory deficits in rats.
化学情報
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CAS 番号 202646-80-8
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性状 Solid
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分子量 385.46
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分子式 C23H23N5O
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Color White to light yellow
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SMILES
O=C1C=CC(C2=C3C=CC=CN3N=C2C4=CC=CC=C4)=NN1C5CCN(CC5)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 2 mg/mL (5.19 mM; Need ultrasonic and warming; 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. 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. 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)
The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.
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.
Working solution concentration: 0.22 mg/mL
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)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Kuroda S, et al. Design, synthesis and biological evaluation of a novel series of potent, orally active adenosine A1 receptor antagonists with high blood-brain barrier permeability. Chem Pharm Bull (Tokyo). 2001 Aug;49(8):988-98. [Content Brief]
[2]. Maemoto T, et al. Pharmacological characterization of FR194921, a new potent, selective, and orally active antagonist for central adenosine A1 receptors. J Pharmacol Sci. 2004 Sep;96(1):42-52. [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. 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 | 2.5943 mL | 12.9715 mL | 25.9430 mL | 64.8576 mL |
| 5 mM | 0.5189 mL | 2.5943 mL | 5.1886 mL | 12.9715 mL |