| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| 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].
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| ln Vivo |
AMPK activator 4 (100 mg/kg; administered intragastrically; daily for 9 weeks) exhibits anti-hyperglycemic properties[1].
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| 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]. Sun G, You Y, Li H, et al. Discovery of AdipoRon analogues as novel AMPK activators without inhibiting mitochondrial complex I. Eur J Med Chem. 2020;200:112466.
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| Molecular Formula |
C24H21CLN2O3
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|---|---|
| Molecular Weight |
420.89
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| CAS # |
2493239-46-4
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| SMILES |
ClC1C=CC(=CC=1)OC(C(NC1C=CC(=CC=1)OCC1C=CC(C#N)=CC=1)=O)(C)C
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| Solubility (In Vitro) |
DMSO : 250 mg/mL (593.98 mM)
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|---|---|
| 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.
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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