PF-06685249
Based on 1 Customer Validation
PF-06685249 (PF-249) is a potent and orally active allosteric AMPK activator with an EC50 of 12 nM for recombinant AMPK α1β1γ1. PF-06685249 improves renal function in ZSF-1 rats with diabetic nephropathy. PF-06685249 can be used for diabetic nephropathy research.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.00%
- CAS No.: 1467059-70-6
- Formule: C17H16ClN3O3
- Masse moléculaire:345.78
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
AMPK α1β1γ1 12 nM (EC50) |
In Vitro
PF-06685249 exhibits potent activating activity against human α1β1γ1-AMPK, with an EC50 of 12 nM and shows high binding affinity to α1β1γ1-AMPK with a KD of 14 nM as determined by SPR experiment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
Parmacokinetics
| Species | Dose | Route | CLplasma | Vss | T1/2 | AUC0-24 | Cmax | Tmax | F |
|---|---|---|---|---|---|---|---|---|---|
| Cynomolgus Monkey[1] | 1 mg/kg | i.v. | 0.98 mL/min/kg | 0.46 L/kg | 9.14 h | 15500 ng·h/mL | / | / | / |
| Cynomolgus Monkey[1] | 3 mg/kg | p.o. | / | / | / | 31200 ng·h/mL | 2540 ng/mL | 1.5 h | 67 % |
| Rat[1] | 1 mg/kg | i.v. | 22.6 mL/min/kg | 0.31 L/kg | 27.2 h | 254000 ng·h/mL | / | / | / |
| Rat[1] | 3 mg/kg | p.o. | / | / | / | 160000 ng·h/mL | 10200 ng/mL | 5.5 h | 52 % |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:ZSF-1 rats (obese/diabetic nephropathy model)[1]
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Dosage:30 mg/kg, 100 mg/kg
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Administration:po, once daily for 3 or 68 days
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Result:Increased the ratio of phosphorylated AMPK (pAMPK) to total AMPK (tAMPK) in renal pole tissue of ZSF-1 rats.
Improved renal function in ZSF-1 rats with diabetic nephropathy after 68 days of continuous administration.
Chemical Information
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CAS No. 1467059-70-6
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Appearance Solid
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Masse moléculaire 345.78
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Formule C17H16ClN3O3
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Color Off-white to gray
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SMILES
O=C(C1=CNC2=C1C=C(C3=CC=C(N(C)C)N=C3OC)C(Cl)=C2)O
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Synonyms
PF-249
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (289.20 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 (275 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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Instruction de manipulation (2659 KB)
Références
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 | 2.8920 mL | 14.4601 mL | 28.9201 mL | 72.3003 mL |
| 5 mM | 0.5784 mL | 2.8920 mL | 5.7840 mL | 14.4601 mL | |
| 10 mM | 0.2892 mL | 1.4460 mL | 2.8920 mL | 7.2300 mL | |
| 15 mM | 0.1928 mL | 0.9640 mL | 1.9280 mL | 4.8200 mL | |
| 20 mM | 0.1446 mL | 0.7230 mL | 1.4460 mL | 3.6150 mL | |
| 25 mM | 0.1157 mL | 0.5784 mL | 1.1568 mL | 2.8920 mL | |
| 30 mM | 0.0964 mL | 0.4820 mL | 0.9640 mL | 2.4100 mL | |
| 40 mM | 0.0723 mL | 0.3615 mL | 0.7230 mL | 1.8075 mL | |
| 50 mM | 0.0578 mL | 0.2892 mL | 0.5784 mL | 1.4460 mL | |
| 60 mM | 0.0482 mL | 0.2410 mL | 0.4820 mL | 1.2050 mL | |
| 80 mM | 0.0362 mL | 0.1808 mL | 0.3615 mL | 0.9038 mL | |
| 100 mM | 0.0289 mL | 0.1446 mL | 0.2892 mL | 0.7230 mL |
PF-06685249 Related Classifications
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