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AMPKactivator 4

Cat No.:V52420 Purity: ≥98%
AMPK activator 4 is a potent AMPK activator and does not inhibit mitochondrial complex I.
AMPKactivator 4
AMPKactivator 4 Chemical Structure CAS No.: 2493239-46-4
Product category: AMPK
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
AMPK activator 4 is a potent AMPK activator and does not inhibit mitochondrial complex I. AMPK activator 4 selectively activates AMPK in muscle tissue. AMPK activator 4 dose-dependently improved glucose tolerance in normal mice, significantly reduced fasting blood glucose levels and improved insulin resistance in db/db diabetic mice. Has hypoglycemic effect.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
AMPK activator 4 (compound B10) (0–20 μM; 12–24 hours) causes AMPK and its downstream protein ACC to become phosphorylated[1]. LKB1 is necessary for AMPK phosphorylation mediated by AMPK activator 4[1]. When HepG2 cells are treated with AMPK activator 4 at 10–20 μM for 72 hours, their viability is slightly decreased[1].
ln Vivo
AMPK activator 4 (100 mg/kg; administered intragastrically; daily for 9 weeks) exhibits anti-hyperglycemic properties[1].
Cell Assay
Western Blot Analysis[1]
Cell Types: C2C12 myotubes, HepG2 and HuH-7 cells
Tested Concentrations: 0-20 μM
Incubation Duration: 12-24 hrs (hours)
Experimental Results: Induced dose-dependently phosphorylation of ACC in C2C12 myotube cells, and the phosphorylation of ACC was highly consistent with the phosphorylation of AMPK. Increased the phosphorylation of AMPK and ACC in human hepatocarcinoma HepG2 and HuH-7 cells.
Animal Protocol
Animal/Disease Models: db/db mice (5-week old)[1]
Doses: 100 mg/kg
Route of Administration: intragastric (po)administration; daily for 9 weeks
Experimental Results: Dramatically lowered the fasting blood glucose in db/db mice (2-6 weeks). Dramatically improved insulin resistance in db /db mice (for 9 weeks). The body weight and the serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) (two markers of liver injury) were not Dramatically affected.
References

[1]. Discovery of AdipoRon analogues as novel AMPK activators without inhibiting mitochondrial complex I. Eur J Med Chem. 2020;200:112466.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H21CLN2O3
Molecular Weight
420.888145208359
Exact Mass
420.124
CAS #
2493239-46-4
PubChem CID
154573764
Appearance
White to off-white solid powder
LogP
5.2
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
4
Rotatable Bond Count
7
Heavy Atom Count
30
Complexity
593
Defined Atom Stereocenter Count
0
SMILES
ClC1C=CC(=CC=1)OC(C(NC1C=CC(=CC=1)OCC1C=CC(C#N)=CC=1)=O)(C)C
InChi Key
OSSMPMZJYDZMFX-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H21ClN2O3/c1-24(2,30-22-11-7-19(25)8-12-22)23(28)27-20-9-13-21(14-10-20)29-16-18-5-3-17(15-26)4-6-18/h3-14H,16H2,1-2H3,(H,27,28)
Chemical Name
2-(4-chlorophenoxy)-N-[4-[(4-cyanophenyl)methoxy]phenyl]-2-methylpropanamide
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)
DMSO : 250 mg/mL (593.98 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3759 mL 11.8796 mL 23.7592 mL
5 mM 0.4752 mL 2.3759 mL 4.7518 mL
10 mM 0.2376 mL 1.1880 mL 2.3759 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.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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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