PF-05085727
Based on 1 Customer Validation
PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11.
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- Purity: 99.53%
- CAS No.: 1415637-72-7
- 화학식: C20H18F3N7
- 분자량:413.40
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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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PDE2A 2 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf21 | IC50 |
2.3 nM
Compound: 1
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Inhibition of full length recombinant human PDE2A expressed in Sf21 cells using [3H]-cGMP as substrate by scintillation proximity assay
Inhibition of full length recombinant human PDE2A expressed in Sf21 cells using [3H]-cGMP as substrate by scintillation proximity assay
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[PMID: 23651455] |
PF-05085727 shows weak activity with IC50 of 162 μM to induce cell death in a cellular toxicity assay using transformed human liver endothelial (THLE) cells[1].PF-05085727 (3 μM) shows a minimal inhibition of cytochrome P450 enzymes (CYPs), inhibits 1A2, 2C8, 2C9, 2D6 and 3A4 with percentage% of 16%, 18%, 7%, 4%, and 30%, respectively[1].PF-05085727 (10 μM) inhibits PDE1B, PDE4B, PDE7B and PDE10A with IC50 values of 12.146 μM, 22,503 μM, 13.157 μM and 6.515 μM, respectively[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.
Chemical Information
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CAS No. 1415637-72-7
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Appearance Solid
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분자량 413.40
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화학식 C20H18F3N7
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Color White to yellow
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SMILES
CN1C2=NC=NC(N3CCC3)=C2C(C4=C(C5=CC=C(C(F)(F)F)C=C5)N(C)N=C4)=N1
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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 2 years -20°C 1 year
용액&용해도
DMSO : 62.5 mg/mL (151.19 mM; Need ultrasonic; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4190 mL | 12.0948 mL | 24.1896 mL | 60.4741 mL |
| 5 mM | 0.4838 mL | 2.4190 mL | 4.8379 mL | 12.0948 mL | |
| 10 mM | 0.2419 mL | 1.2095 mL | 2.4190 mL | 6.0474 mL | |
| 15 mM | 0.1613 mL | 0.8063 mL | 1.6126 mL | 4.0316 mL | |
| 20 mM | 0.1209 mL | 0.6047 mL | 1.2095 mL | 3.0237 mL | |
| 25 mM | 0.0968 mL | 0.4838 mL | 0.9676 mL | 2.4190 mL | |
| 30 mM | 0.0806 mL | 0.4032 mL | 0.8063 mL | 2.0158 mL | |
| 40 mM | 0.0605 mL | 0.3024 mL | 0.6047 mL | 1.5119 mL | |
| 50 mM | 0.0484 mL | 0.2419 mL | 0.4838 mL | 1.2095 mL | |
| 60 mM | 0.0403 mL | 0.2016 mL | 0.4032 mL | 1.0079 mL | |
| 80 mM | 0.0302 mL | 0.1512 mL | 0.3024 mL | 0.7559 mL | |
| 100 mM | 0.0242 mL | 0.1209 mL | 0.2419 mL | 0.6047 mL |
PF-05085727 Related Classifications
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