PF 750
Based on 1 Customer Validation
PF 750 is a selective, covalent and brain-penetrant fatty acid amide hydrolase (FAAH) inhibitor. PF 750 covalently carbamylates FAAH's catalytic serine nucleophile to inactivate the enzyme.
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- Pureté: 98.99%
- CAS No.: 959151-50-9
- Formule: C22H23N3O
- Masse moléculaire:345.44
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
IC50: 16.2-595 nM (FAAH)[1].
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
17 nM
Compound: 8, PF-750
|
Inhibition of rat FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay
Inhibition of rat FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay
|
10.1039/C2MD00307D |
| HEK293 | IC50 |
4.6 nM
Compound: 8, PF-750
|
Inhibition of human FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay
Inhibition of human FAAH expressed in HEK293 cells using arachadonyl 7-amino 4-methyl coumarin amide as substrate by fluorimetric assay
|
10.1039/C2MD00307D |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild-type mice[2]
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Dosage:10, 30 mg/kg
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Administration:i.p., single dose
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Result:Selectively targeted FAAH in the brain and showed no detectable off-target activity in peripheral tissues.
Chemical Information
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CAS No. 959151-50-9
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Appearance Solid
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Masse moléculaire 345.44
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Formule C22H23N3O
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Color White to off-white
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SMILES
O=C(NC1=CC=CC=C1)N(CC2)CCC2CC3=CN=C4C(C=CC=C4)=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (289.49 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, 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)
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Ahn K, et al. Discovery and characterization of a highly selective FAAH inhibitor that reduces inflammatory pain. Chem Biol. 2009;16(4):411-420. [Content Brief]
[2]. Ahn K, Johnson DS, et al. Novel mechanistic class of fatty acid amide hydrolase inhibitors with remarkable selectivity. Biochemistry. 2007 Nov 13;46(45):13019-30. [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 | 2.8949 mL | 14.4743 mL | 28.9486 mL | 72.3715 mL |
| 5 mM | 0.5790 mL | 2.8949 mL | 5.7897 mL | 14.4743 mL | |
| 10 mM | 0.2895 mL | 1.4474 mL | 2.8949 mL | 7.2371 mL | |
| 15 mM | 0.1930 mL | 0.9650 mL | 1.9299 mL | 4.8248 mL | |
| 20 mM | 0.1447 mL | 0.7237 mL | 1.4474 mL | 3.6186 mL | |
| 25 mM | 0.1158 mL | 0.5790 mL | 1.1579 mL | 2.8949 mL | |
| 30 mM | 0.0965 mL | 0.4825 mL | 0.9650 mL | 2.4124 mL | |
| 40 mM | 0.0724 mL | 0.3619 mL | 0.7237 mL | 1.8093 mL | |
| 50 mM | 0.0579 mL | 0.2895 mL | 0.5790 mL | 1.4474 mL | |
| 60 mM | 0.0482 mL | 0.2412 mL | 0.4825 mL | 1.2062 mL | |
| 80 mM | 0.0362 mL | 0.1809 mL | 0.3619 mL | 0.9046 mL | |
| 100 mM | 0.0289 mL | 0.1447 mL | 0.2895 mL | 0.7237 mL |