PF-06445974
Based on 1 Customer Validation
PF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study.
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: 98.59%
- CAS 番号: 2055776-17-3
- 分子式: C20H15FN4O
- 分子量:346.36
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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生物活性
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PDE4B <1 nM (IC50) |
PDE4D 36 nM (IC50) |
PDE4A 4.7 nM (IC50) |
PDE4C 17 nM (IC50) |
PF-06445974 demonstrates minimal off-target activities in broad-spectrum selectivity panels, with only weak µM activities at PDE10 (IC50=2290 nM), PDE5A (IC50=4640 nM) and GABAA (Ki=3850 nM)[1].
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.
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Animal Model:Twenty-five drug-naive male 129/B6 PDE4D KO mice (25-35 g)[1]
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Dosage:10 µg/kg
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Administration:Dosed intravenously at 10 µg/kg in a 5 mL/kg dosing volume
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Result:Showed excellent brain uptake and reached peak concentrations at around 20 minutes.
化学情報
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CAS 番号 2055776-17-3
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性状 Solid
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分子量 346.36
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分子式 C20H15FN4O
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Color White to off-white
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SMILES
N#CC1=CC=C(C=C1F)C2=C(C3=O)N(CCN3C4CC4)C5=CC=CN=C25
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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 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 33.33 mg/mL (96.23 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. 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)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 2.8872 mL | 14.4358 mL | 28.8717 mL | 72.1792 mL |
| 5 mM | 0.5774 mL | 2.8872 mL | 5.7743 mL | 14.4358 mL | |
| 10 mM | 0.2887 mL | 1.4436 mL | 2.8872 mL | 7.2179 mL | |
| 15 mM | 0.1925 mL | 0.9624 mL | 1.9248 mL | 4.8119 mL | |
| 20 mM | 0.1444 mL | 0.7218 mL | 1.4436 mL | 3.6090 mL | |
| 25 mM | 0.1155 mL | 0.5774 mL | 1.1549 mL | 2.8872 mL | |
| 30 mM | 0.0962 mL | 0.4812 mL | 0.9624 mL | 2.4060 mL | |
| 40 mM | 0.0722 mL | 0.3609 mL | 0.7218 mL | 1.8045 mL | |
| 50 mM | 0.0577 mL | 0.2887 mL | 0.5774 mL | 1.4436 mL | |
| 60 mM | 0.0481 mL | 0.2406 mL | 0.4812 mL | 1.2030 mL | |
| 80 mM | 0.0361 mL | 0.1804 mL | 0.3609 mL | 0.9022 mL |
PF-06445974 関連分類
HY-119190 関連分類
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