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AMPK activator 12

Cat No.:V55742 Purity: ≥98%
AMPK activator 12 (compound 21) is a potent AMPK activator and GDF15 inducer.
AMPK activator 12
AMPK activator 12 Chemical Structure CAS No.: 431920-24-0
Product category: AMPK
This product is for research use only, not for human use. We do not sell to patients.
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10mg
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100mg
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Product Description
AMPK activator 12 (compound 21) is a potent AMPK activator and GDF15 inducer. AMPK activator 12 increases GDF15 protein levels in human hepatocytes.
AMPK activator 12 (compound 21) is a potent activator of AMP-activated protein kinase (AMPK) and an inducer of growth differentiation factor 15 (GDF15). It increases GDF15 protein levels in human hepatic cells. AMPK activation and GDF15 induction have implications for cancer research and metabolic diseases. It is a research-grade compound not approved for human therapeutic use.
Biological Activity I Assay Protocols (From Reference)
Targets
AMPK (AMP-activated protein kinase). AMPK activator 12 is a potent AMPK activator. It also induces GDF15 expression. AMPK is a key energy sensor that regulates cellular metabolism, autophagy, and cell growth. GDF15 is a cytokine involved in energy homeostasis and cancer.
ln Vitro
AMPK activator 12 demonstrates potent activation of AMPK in biochemical and cellular assays. It increases GDF15 protein levels in human hepatic cells. The compound's dual activity as an AMPK activator and GDF15 inducer makes it a valuable tool for studying energy metabolism and cancer pathways. Detailed EC50 values have not been disclosed.
ln Vivo
In vivo activity of AMPK activator 12 has not been extensively characterized in published literature. The compound is primarily used as an in vitro research tool. In vivo studies would be needed to evaluate its therapeutic potential in cancer or metabolic disease models. Currently, no in vivo efficacy data have been reported in peer-reviewed literature.
Enzyme Assay
In vitro enzyme assays for AMPK activation are performed using recombinant AMPK enzyme and a suitable peptide substrate (e.g., SAMS peptide) in the presence of ATP. AMPK activator 12 is incubated at varying concentrations with the enzyme and substrate. Phosphorylation is detected by radioactivity (³³P-ATP) or by fluorescence-based methods (e.g., ADP-Glo). EC50 values are calculated from dose-response curves. For GDF15 induction, ELISA or Western blot is used.
Cell Assay
Cells (e.g., human hepatic cells, hepatocytes, or cancer cell lines) are cultured and treated with AMPK activator 12 at concentrations ranging from 0.1–50 μM for 24–72 hours. AMPK activation is assessed by measuring phosphorylation of AMPK and its downstream targets (e.g., ACC) by Western blot. GDF15 protein levels are measured by ELISA or Western blot. Cell viability and proliferation are evaluated by standard assays.
Animal Protocol
In vivo animal studies for AMPK activator 12 have not been reported in publicly available literature. The compound is primarily used for in vitro research. Future studies in animal models of cancer or metabolic diseases would be needed to evaluate in vivo efficacy. Standard protocols for AMPK activator studies could be adapted.
ADME/Pharmacokinetics
Pharmacokinetic data for AMPK activator 12 have not been published. The compound has a molecular weight of 426.35 and formula C23H24BrNO2. Solubility information is limited. In vivo PK parameters such as half-life, bioavailability, and tissue distribution have not been characterized. For in vivo use, formulation would need to be developed.
Toxicity/Toxicokinetics
Toxicology data for AMPK activator 12 have not been published. The compound is for research use only and not approved for human therapeutic applications. No systematic toxicological evaluation has been performed. Standard safety precautions for handling chemical activators should be observed.
References

[1]. Design and Synthesis of AMPK Activators and GDF15 Inducers. Molecules. 2023 Jul 17;28(14):5468.

Additional Infomation
AMPK activator 12 (CAS: 431920-24-0, molecular formula C23H24BrNO2, molecular weight 426.35) is also known as compound 21. It is a potent AMPK activator and GDF15 inducer. It is not in clinical trials and has no regulatory approval. The compound is supplied as a research-grade activator for laboratory use only.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Exact Mass
425.099
CAS #
431920-24-0
PubChem CID
2910412
Appearance
White to off-white solid powder
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
9
Heavy Atom Count
27
Complexity
368
Defined Atom Stereocenter Count
0
SMILES
C1=CC=C(C=C1)CN(CC2=CC=CC=C2)CC(COC3=CC=C(C=C3)Br)O
InChi Key
WNGGJGGXJPRFJK-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H24BrNO2/c24-21-11-13-23(14-12-21)27-18-22(26)17-25(15-19-7-3-1-4-8-19)16-20-9-5-2-6-10-20/h1-14,22,26H,15-18H2
Chemical Name
1-(4-bromophenoxy)-3-(dibenzylamino)propan-2-ol
HS Tariff Code
2934.99.9001
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)
Solubility Data
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
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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