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| Targets |
The primary target of PF-07293893 is the gamma3 subunit of AMP‑activated protein kinase (AMPK). AMPK is a heterotrimeric enzyme composed of alpha (catalytic), beta (regulatory), and gamma (regulatory/substrate-binding) subunits. The gamma3 isoform is predominantly expressed in skeletal muscle. PF-07293893 binds specifically to the gamma3 subunit, activating the kinase complex in an isoform-selective manner. The activation of AMPK leads to an increase in cellular ATP production and a decrease in ATP consumption. This has potential benefits in metabolic disorders and heart failure.
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| ln Vitro |
In vitro, PF-07293893 is a selective AMPK gamma3 activator. It binds to the gamma3 subunit of the AMPK complex, leading to its activation. The exact in vitro potency (EC₅0) for AMPK activation has not been specified in the provided data. The activation of AMPK results in the phosphorylation of downstream targets such as acetyl-CoA carboxylase (ACC), leading to increased fatty acid oxidation and inhibition of fatty acid synthesis. The selectivity for gamma3 over other AMPK isoforms is a key aspect of its profile.
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| ln Vivo |
In vivo, PF-07293893 is an activator of AMPK gamma3 and is used in heart failure research. In animal models of heart failure, AMPK activation has been shown to improve cardiac function and energy metabolism. While specific in vivo data for PF-07293893 are not provided, the compound is being studied for its potential therapeutic benefits in cardiovascular diseases.
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| Enzyme Assay |
Non-cell-based (cell-free) experiments for PF-07293893 use purified recombinant AMPK complexes containing the gamma3 subunit. A standard protocol involves incubating the enzyme with increasing concentrations of the compound (0.1-1000 nM) in the presence of ATP and a fluorescently labeled peptide substrate (e.g., an AMARA or SAMS peptide). The reaction proceeds for 30-60 minutes at 37degC. The kinase activity is measured by detecting the phosphorylation of the substrate using a fluorescence polarization (FP) or homogeneous time-resolved fluorescence (HTRF) assay. The EC₅0 for AMPK activation is calculated. The specificity is confirmed by testing the compound against other AMPK isoform complexes (alpha1beta1gamma1, alpha2beta1gamma1, alpha2beta2gamma1).
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| Cell Assay |
Cell-based assays for PF-07293893 are conducted in cell lines that express the AMPK gamma3 isoform, such as L6 rat myotubes or human skeletal muscle myotubes. Cells are treated with increasing concentrations of the compound (0.01-10 uM) for 1-6 hours. After treatment, the cells are lysed, and the activation of AMPK is measured by Western blotting for phosphorylation of AMPK at Thr172 (a marker of activation) and phosphorylation of its downstream target acetyl-CoA carboxylase (ACC) at Ser79. The EC₅0 is calculated from densitometric analysis of the bands. Metabolic readouts such as glucose uptake (by 2‑deoxyglucose uptake assay) and fatty acid oxidation (by 14C‑oleate oxidation) can also be assessed.
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| Animal Protocol |
In vivo animal experiments for PF-07293893 are conducted in rodent models of metabolic or cardiovascular disease. In a heart failure model, rats are subjected to transverse aortic constriction (TAC) or myocardial infarction to induce heart failure. PF-07293893 is administered orally at doses of 1-100 mg/kg once daily for 4-8 weeks. Cardiac function is assessed by echocardiography (ejection fraction, fractional shortening) and pressure‑volume (PV) loop analysis. Endpoints include heart weight, plasma NT‑proBNP levels, and histology (fibrosis). Metabolic parameters such as plasma glucose, insulin, and triglycerides are also measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for PF-07293893 are not available in the provided material. The compound has a molecular formula of C2₆H23ClF4N₆O2 and a molecular weight of 562.95 g/mol. It is stored under the recommended conditions in the certificate of analysis. The product is for research use only.
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| Toxicity/Toxicokinetics |
The toxicity of PF-07293893 has not been characterized. As a research chemical, standard safety precautions apply: the compound may be harmful if swallowed, inhaled, or absorbed through the skin. It may cause skin and eye irritation. It should be handled in a well-ventilated area (fume hood) with appropriate PPE (lab coat, gloves, safety goggles). The product is not for human or veterinary use.
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| References | |
| Additional Infomation |
Additional information: The compound has a CAS number of 3036759-47-1. It is also known as PF07293893 and PF 07293893. It is selective AMPK gamma3 activator for heart failure research. The product is for research use only.
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| Molecular Formula |
C26H23CLF4N6O2
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| Molecular Weight |
562.95
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| CAS # |
3036759-47-1
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| Appearance |
White to off-white solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7764 mL | 8.8818 mL | 17.7636 mL | |
| 5 mM | 0.3553 mL | 1.7764 mL | 3.5527 mL | |
| 10 mM | 0.1776 mL | 0.8882 mL | 1.7764 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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