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.
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- Pureza: 98.54%
- No. CAS: 202646-80-8
- Fòrmula: C23H23N5O
- Peso molecular:385.46
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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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.
Chemical Information
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No. CAS 202646-80-8
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Appearance Solid
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Peso molecular 385.46
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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
Pureza y Documentación
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Ficha de datos (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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Instrucciones de manejo (2659 KB)
Referencias
[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 |