PF-06409577
Based on 1 publication(s) in Google Scholar
PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.83%
- No. CAS: 1467057-23-3
- Fòrmula: C19H16ClNO3
- Peso molecular:341.79
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) PF-06409577
MoreVer todos los productos específicos de isoformas AMPK
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Actividad biológica
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AMPK α1β1γ1 7 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>30000 nM
Compound: 7
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Agonist activity at human recombinant 5-HT2b receptor expressed in CHO cells measured after 30 mins by HTRF assay
Agonist activity at human recombinant 5-HT2b receptor expressed in CHO cells measured after 30 mins by HTRF assay
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[PMID: 27490827] |
| Sf9 | EC50 |
>40 μM
Compound: 29; PF-06409577
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Activation of rat hepatocytes AMPK alpha1/beta2/gamma1 expressed in baculovirus infected Sf9 cells
Activation of rat hepatocytes AMPK alpha1/beta2/gamma1 expressed in baculovirus infected Sf9 cells
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[PMID: 31930920] |
| Sf9 | EC50 |
0.007 μM
Compound: 29; PF-06409577
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Activation of rat hepatocytes AMPK alpha1/beta1/gamma1 expressed in baculovirus infected Sf9 cells
Activation of rat hepatocytes AMPK alpha1/beta1/gamma1 expressed in baculovirus infected Sf9 cells
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[PMID: 31930920] |
| Vero | CC50 |
586.4 μM
Compound: 54; PF-06409577
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Cytotoxicity against African green monkey Vero cells after 48 hrs by Cell Titer Glo luminescent cell viability assay
Cytotoxicity against African green monkey Vero cells after 48 hrs by Cell Titer Glo luminescent cell viability assay
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[PMID: 31549836] |
| Vero | CC50 |
923.7 μM
Compound: 54; PF-06409577
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Cytotoxicity against African green monkey Vero cells after 24 hrs by Cell Titer Glo luminescent cell viability assay
Cytotoxicity against African green monkey Vero cells after 24 hrs by Cell Titer Glo luminescent cell viability assay
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[PMID: 31549836] |
| Vero | EC50 |
2.6 μM
Compound: 54; PF-06409577
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Activation of AMPK in African green monkey Vero cells infected with Zika virus PA259459 assessed as antiviral activity measured 24 hrs post infection by plaque assay
Activation of AMPK in African green monkey Vero cells infected with Zika virus PA259459 assessed as antiviral activity measured 24 hrs post infection by plaque assay
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[PMID: 31549836] |
PF-06409577 possesses similar potency toward the human and rat α1β1γ1 isoforms. In broad panel screening against other receptors, channels, PDEs and kinases, PF-06409577 exhibits minimal off-target pharmacology. PF-06409577 shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and is not an inhibitor (IC50>100 μM) of the microsomal activities of major human cytochrome P450 isoforms[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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1467057-23-3
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Appearance Solid
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Peso molecular 341.79
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Fòrmula C19H16ClNO3
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Color White to off-white
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SMILES
O=C(C1=CNC2=C1C=C(C3=CC=C(C4(O)CCC4)C=C3)C(Cl)=C2)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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mBio
2024 Dec 11;15(12):e0213724. PMID: 39475231
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (292.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
PF-06409577 is prepared in DMSO. PF-06409577 is incubated with fully phosphorylated AMPK in assay buffer at room temperature for 15 min followed by addition of PP2a and another incubation for 60 min at room temperature. The phosphatase treatment is quenched and the kinase assay initiated with the addition of okadaic acid (50 nM final), 50 nM Cy-5 SAMS peptide and ATP equal to Km for each isoform. Reactions are incubated for an additional 60 min and the kinase reaction is quenched with the addition of 10 mM EDTA and 2 nM Eu-pACC antibody in detection Buffer. Kinase activity is monitored by excitation at 320 nM and measuring emission at 665 and 615 nM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Rats: Daily administration of 0.5% methylcellulose (p.o.), PF-06409577 at 10, 30, or 100 mg/kg (p.o.), PF- 249 at 3, 10, or 30 mg/kg (p.o.), or ramipril in drinking water (1 mg/kg/day) is initiated and continued for 68 days. Urine is collected for 24-hours and volume recorded from all lean and obese rats after 14, 28, 42, and 60 days of dosing. On Day 63 all rats are administered a final dose after 16-hour overnight fasting. One hour following the final dose, blood glucose is measured by glucometer and a 100 μL tail vein blood sample collected and processed for determination of insulin levels and total protein. Each rat is then anesthetized with isoflurane. The right kidney is collected and immediately freeze-clamped and transferred to liquid nitrogen storage; the left kidney is fixed in 10% formalin. Rats are then euthanized by exsanguination from the vena cava[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (281 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Cameron KO, et al. Discovery and Preclinical Characterization of 6-Chloro-5-[4-(1-hydroxycyclobutyl)phenyl]-1H-indole-3-carboxylic Acid (PF-06409577), a Direct Activator of Adenosine Monophosphate-activated Protein Kinase (AMPK), for the Potential Treatment of Diabetic Nephropathy. J Med Chem. 2016 Sep 8;59(17):8068-81. [Content Brief]
[2]. Salatto CT, et al. Selective Activation of AMPK β1-Containing Isoforms Improves Kidney Function in a Rat Model of Diabetic Nephropathy. J Pharmacol Exp Ther. 2017 May;361(2):303-311. [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, 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 | 2.9258 mL | 14.6289 mL | 29.2577 mL | 73.1443 mL |
| 5 mM | 0.5852 mL | 2.9258 mL | 5.8515 mL | 14.6289 mL | |
| 10 mM | 0.2926 mL | 1.4629 mL | 2.9258 mL | 7.3144 mL | |
| 15 mM | 0.1951 mL | 0.9753 mL | 1.9505 mL | 4.8763 mL | |
| 20 mM | 0.1463 mL | 0.7314 mL | 1.4629 mL | 3.6572 mL | |
| 25 mM | 0.1170 mL | 0.5852 mL | 1.1703 mL | 2.9258 mL | |
| 30 mM | 0.0975 mL | 0.4876 mL | 0.9753 mL | 2.4381 mL | |
| 40 mM | 0.0731 mL | 0.3657 mL | 0.7314 mL | 1.8286 mL | |
| 50 mM | 0.0585 mL | 0.2926 mL | 0.5852 mL | 1.4629 mL | |
| 60 mM | 0.0488 mL | 0.2438 mL | 0.4876 mL | 1.2191 mL | |
| 80 mM | 0.0366 mL | 0.1829 mL | 0.3657 mL | 0.9143 mL | |
| 100 mM | 0.0293 mL | 0.1463 mL | 0.2926 mL | 0.7314 mL |
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