| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
AMPK activator 1 targets AMP-activated protein kinase (AMPK), a heterotrimeric serine/threonine protein kinase composed of alpha (catalytic), beta (regulatory), and gamma (regulatory) subunits. AMPK is activated by increases in the cellular AMP/ATP and ADP/ATP ratios, signaling energy depletion. Activated AMPK phosphorylates downstream targets to promote catabolic pathways (glucose uptake, fatty acid oxidation, mitochondrial biogenesis) and inhibit anabolic pathways (lipogenesis, protein synthesis, gluconeogenesis). AMPK is a master regulator of cellular energy balance and is a therapeutic target for metabolic diseases including type 2 diabetes, obesity, and non-alcoholic fatty liver disease. AMPK activator 1 activates AMPK with an EC₅0 of <0.1 microM.
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| ln Vitro |
AMPK Activator 1 (Compound No. 1-75) uses an enzyme-linked immunosorbent test to activate AMPK [1].
In vitro, AMPK activator 1 activates AMPK with an EC₅0 of less than 0.1 microM. The compound activates AMPK using an enzyme-linked immunosorbent assay (ELISA)-based method. In cellular assays, AMPK activator 1 increases AMPK phosphorylation at Thr172 (the activation loop) and enhances phosphorylation of downstream AMPK substrates such as acetyl-CoA carboxylase (ACC) and ULK1. The compound is used to study the cellular effects of AMPK activation on metabolic pathways, including glucose uptake, fatty acid oxidation, and autophagy. AMPK activator 1 has shown significant potential in research applications in metabolism, obesity, diabetes, and cancer studies. |
| ln Vivo |
In vivo data for AMPK activator 1 are limited as the compound is primarily described in a patent for AMPK activators. The compound has not been extensively characterized in animal models. However, AMPK activation in vivo is known to improve insulin sensitivity, reduce blood glucose, promote weight loss, and exert anticancer effects. The compound is intended for research use only and has not been evaluated in clinical trials. The pharmacokinetic properties, bioavailability, and tissue distribution of AMPK activator 1 have not been characterized. Researchers should consult the primary literature and patent for the most current information.
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| Enzyme Assay |
In vitro enzyme assays for AMPK activator 1 involve measuring AMPK activity using recombinant human AMPK enzyme or cell lysates. The assay is typically performed in 96-well or 384-well plates using a kinase assay format. AMPK is incubated with ATP and a peptide substrate (e.g., a biotinylated peptide derived from ACC or SAMS peptide) in assay buffer. Serial dilutions of AMPK activator 1 (0.001-10 microM) are added to the reaction. After incubation at 30degC for 30-60 minutes, kinase activity is quantified by measuring phosphorylation of the substrate using a fluorescence-based, luminescence-based (ADP-Glo), or radioactivity-based detection system. EC₅0 values are determined from dose-response curves using nonlinear regression.
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| Cell Assay |
Cellular assays for AMPK activator 1 are performed using cell lines such as HepG2 (hepatoma), L6 (myotubes), or 3T3-L1 (adipocytes). Cells are cultured in appropriate medium and seeded in 6- or 96-well plates. Cells are treated with serial dilutions of AMPK activator 1 (0.001-10 microM) for 1-24 hours. AMPK activation is assessed by Western blotting for phospho-AMPK (Thr172) and phospho-ACC (Ser79) or other downstream substrates. Cellular metabolic readouts include glucose uptake (using 2-NBDG or [3H]-2-deoxyglucose), fatty acid oxidation (using [14C]-palmitate), and mitochondrial function (oxygen consumption rate). Cell viability and proliferation are monitored. The compound's effects on metabolic pathways are characterized.
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| Animal Protocol |
In vivo animal studies for AMPK activator 1 have not been extensively reported. The compound is identified from a patent for AMPK activators. For in vivo studies, researchers may consider administering the compound to rodent models of metabolic disease (e.g., diet-induced obesity, db/db mice, STZ-induced diabetes) at doses determined by pharmacokinetic studies. Parameters such as blood glucose, insulin sensitivity, body weight, and lipid profiles would be monitored. Tissue AMPK phosphorylation would be assessed. However, specific protocols and dosing regimens have not been established. Researchers should consult the patent and primary literature for the most current information.
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| ADME/Pharmacokinetics |
AMPK activator 1 (CAS#: 1152423-98-7) has molecular formula C32H33F3N4O3 and molecular weight 578.62. The compound is identified as compound No. 1-75 from patent WO2013116491A1. It is a potent AMPK activator with an EC₅0 of less than 0.1 microM. The compound is a research chemical for laboratory use only, not for human therapeutic applications. It is used in research to study the role of AMPK in cellular metabolism, energy homeostasis, and disease. The compound should be stored at -20degC and is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Toxicological information for AMPK activator 1 is limited as the compound is a research chemical. Based on its mechanism of AMPK activation, potential effects may include hypoglycemia, altered lipid metabolism, and effects on cell growth. The compound should be handled with standard laboratory precautions including the use of personal protective equipment and working in a well-ventilated area. Avoid inhalation, ingestion, and skin contact. The compound should be stored at -20degC and disposed of according to institutional guidelines for chemical waste.
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| References | |
| Additional Infomation |
AMPK activator 1 (CAS#: 1152423-98-7) is a potent activator of AMP-activated protein kinase (AMPK) with an EC₅0 of less than 0.1 microM. The compound is identified as compound No. 1-75 from patent WO2013116491A1 and is used as a representative AMPK activator for research purposes. AMPK is a master regulator of cellular energy homeostasis and a therapeutic target for metabolic diseases including type 2 diabetes, obesity, and cancer. AMPK activator 1 is used in research to study the cellular and physiological effects of AMPK activation on metabolism, energy balance, and disease. The compound is supplied for research use only and is not approved for clinical use. As of the current date, AMPK activator 1 remains a preclinical research compound.
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| Molecular Formula |
C32H33F3N4O3
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| Molecular Weight |
578.6246
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| Exact Mass |
578.25
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| CAS # |
1152423-98-7
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| PubChem CID |
42629942
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| Appearance |
White to off-white solid powder
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| LogP |
6.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
42
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| Complexity |
864
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC(C1C([H])=C([H])C(=C([H])C=1[H])N1C([H])([H])C([H])([H])C([H])(C([H])([H])C1([H])[H])OC1C([H])=C([H])C2=C(C([H])=C(C(N([H])C3([H])C([H])([H])C([H])([H])N(C([H])([H])C4C([H])=C([H])N=C([H])C=4[H])C([H])([H])C3([H])[H])=O)O2)C=1[H])(F)F
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| InChi Key |
LKEAXBYFCTZTLD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H33F3N4O3/c33-32(34,35)24-1-3-26(4-2-24)39-17-11-27(12-18-39)41-28-5-6-29-23(19-28)20-30(42-29)31(40)37-25-9-15-38(16-10-25)21-22-7-13-36-14-8-22/h1-8,13-14,19-20,25,27H,9-12,15-18,21H2,(H,37,40)
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| Chemical Name |
N-[1-(pyridin-4-ylmethyl)piperidin-4-yl]-5-[1-[4-(trifluoromethyl)phenyl]piperidin-4-yl]oxy-1-benzofuran-2-carboxamide
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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) |
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 | 1.7282 mL | 8.6412 mL | 17.2825 mL | |
| 5 mM | 0.3457 mL | 1.7282 mL | 3.4565 mL | |
| 10 mM | 0.1728 mL | 0.8641 mL | 1.7282 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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