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| Targets |
PF-739 targets AMPK (AMP-activated protein kinase) as a non-selective activator. It activates 12 heterotrimeric AMPK complexes. AMPK is a key regulator of cellular energy homeostasis, and its activation leads to increased glucose uptake, fatty acid oxidation, and mitochondrial biogenesis. The compound is used in metabolic research.
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| ln Vitro |
PF-739 had EC50 values of 5.23 nM, 42.2 nM, 8.99 nM, and 126 nM, respectively, activating α2β1η1, α2β2η1, α1β1η1, and α1β2η1[1]. Primary reserves are increased in an anesthetic way by PF-739 (0-1000 nM). AMPK substrate phosphorylation in primary human cardiomyocyte lines and hepatocyte myotubes [2].
In vitro, PF-739 activates AMPK in hepatocytes and skeletal muscle. It activates 12 heterotrimeric AMPK complexes. The compound is a non-selective AMPK activator. Its effects on glucose metabolism and energy homeostasis are studied in cellular models. |
| ln Vivo |
In C57BL/6 mice's hepatocytes and branch muscles, PF-739 (30–1000 mg/kg; vascular or subcutaneous injection; single dosage) efficiently activates AMPK and decreases vascular levels [2].
In vivo, PF-739 significantly reduces the level of glucose in plasma. It is orally active. The compound is used to investigate therapeutic strategies for metabolic or inflammatory disorders. Specific in vivo efficacy data are limited in the available literature. |
| Enzyme Assay |
Specific cell-free enzyme/receptor binding assay protocols for PF-739 involve AMPK activation assays. AMPK activity is measured using purified AMPK enzyme with appropriate substrates. Activation of 12 heterotrimeric AMPK complexes is confirmed through biochemical assays.
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| Cell Assay |
In vitro cell-based assays for PF-739 use hepatocytes and skeletal muscle cells. Cells are treated with the compound, and AMPK activation is assessed by measuring phosphorylation of AMPK and its downstream targets (e.g., ACC). Glucose uptake and fatty acid oxidation are measured to assess functional effects.
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| Animal Protocol |
Animal/Disease Models: C57BL/6 mice[2].
Doses: 30, 100, 300 or 1000 mg/kg. Mode of Route of Administration: oral administration or subcutaneous injection; if single. Experimental Results: AMPK activity increased in skeletal muscle, AMPK phosphorylation in liver tissue and expression of transcription factors Ppargc1a, Nr4a1, and Nr4a3 in the glucose metabolism pathway increased, and plasma insulin and blood glucose diminished. In vivo animal studies for PF-739 are not extensively detailed. The compound is orally active and reduces plasma glucose levels. Typical in vivo evaluation would involve rodent models of metabolic disorders, with endpoints including blood glucose, insulin sensitivity, and body weight. Specific study protocols are not reported. |
| ADME/Pharmacokinetics |
PF-739 has a molecular formula of C23H23ClN2O5 and a molecular weight of 442.89 g/mol. Purity is ≥98%. The compound is orally active. Storage: dry, dark, at 0-4°C for short term or -20°C for long term. The compound is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Specific toxicological data for PF-739 are not detailed in the available literature. The compound is classified for research use only and is not intended for human therapeutic applications. As an AMPK activator, potential toxicities would relate to effects on energy metabolism, though formal toxicological profiles are not reported.
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| References | |
| Additional Infomation |
PF-739 (CAS 1852452-14-2) is an orally active and non-selective AMPK activator that activates 12 heterotrimeric AMPK complexes and significantly reduces plasma glucose levels. It is used in metabolic research to study AMPK activation and glucose homeostasis. No clinical trial data are available.
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| Molecular Formula |
C23H23CLN2O5
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|---|---|
| Molecular Weight |
442.892125368118
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| Exact Mass |
442.129
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| CAS # |
1852452-14-2
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| PubChem CID |
118640073
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2.7
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
31
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| Complexity |
658
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| Defined Atom Stereocenter Count |
4
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| SMILES |
ClC1=CC2=C(C=C1C1C=CC(=CC=1)C1(CO)CC1)N=C(N2)O[C@@H]1CO[C@@H]2[C@@H](CO[C@@H]21)O
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| InChi Key |
IMVYDTHPRTUISR-XRXFAXGQSA-N
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| InChi Code |
InChI=1S/C23H23ClN2O5/c24-15-8-17-16(7-14(15)12-1-3-13(4-2-12)23(11-27)5-6-23)25-22(26-17)31-19-10-30-20-18(28)9-29-21(19)20/h1-4,7-8,18-21,27-28H,5-6,9-11H2,(H,25,26)/t18-,19-,20-,21-/m1/s1
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| Chemical Name |
(3R,3aR,6R,6aR)-6-[[6-chloro-5-[4-[1-(hydroxymethyl)cyclopropyl]phenyl]-1H-benzimidazol-2-yl]oxy]-2,3,3a,5,6,6a-hexahydrofuro[3,2-b]furan-3-ol
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| Synonyms |
PF739; PF 739; PF-739
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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 |
| 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) |
DMSO: ~100 mg/mL (~225.8 mM; with ultrasonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.64 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.64 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: 2.5 mg/mL (5.64 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2579 mL | 11.2895 mL | 22.5790 mL | |
| 5 mM | 0.4516 mL | 2.2579 mL | 4.5158 mL | |
| 10 mM | 0.2258 mL | 1.1289 mL | 2.2579 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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