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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 98.59%
- CAS No.: 2055776-17-3
- 화학식: C20H15FN4O
- 분자량:346.36
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보관: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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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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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.
Chemical Information
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CAS No. 2055776-17-3
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Appearance Solid
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분자량 346.36
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (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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Handling Instructions (2659 KB)
References
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 Related Classifications
HY-119190 Related Classifications
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