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Purity: ≥98%
EX229 (EX-229; AMPK Activator 991), a benzimidazole analog, is a novel, potent and allosteric AMPK (AMP-activated protein kinase) activator with Kd values of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively. AMPK plays a major role in regulating cellular energy balance by sensing and responding to increases in AMP/ADP concentration relative to ATP. Binding of AMP causes allosteric activation of the enzyme and binding of either AMP or ADP promotes and maintains the phosphorylation of threonine 172 within the activation loop of the kinase. AMPK has attracted widespread interest as a potential therapeutic target for metabolic diseases including type 2 diabetes and, more recently, cancer. EX229 activates AMPK in incubated rat epitrochlearis skeletal muscle and incubation of rat skeletal muscle with ex229 increases glucose uptake. The stimulation of skeletal muscle glucose uptake by ex229 is PI3K/PKB-independent, while AMPK-dependent. ex229 increases fatty acid oxidation and glucose uptake in L6 myotubes.
| Targets |
AMPK α1β1γ1 (Kd = 0.06 μM); AMPK α2β1γ1 (Kd = 0.06 μM); AMPK α1β2γ1 (Kd = 0.51 μM)
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| ln Vitro |
EX229 activates AMPK in incubated rat epitrochlearis skeletal muscle and incubation of rat skeletal muscle with ex229 increases glucose uptake. Ex229 stimulates skeletal muscle glucose uptake, but this stimulation is AMPK-dependent and PI3K/PKB-independent. In L6 myotubes, ex229 boosts fatty acid oxidation and glucose uptake[1].
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| Cell Assay |
Vehicle or 50 μM 991 were applied to cells transfected with Myc-Rabep1 WT or Ser407Ala for 60 min.
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| References |
| Molecular Formula |
C24H18CLN3O3
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| Molecular Weight |
431.8710
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| Exact Mass |
431.103
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| Elemental Analysis |
C, 66.75; H, 4.20; Cl, 8.21; N, 9.73; O, 11.11
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| CAS # |
1219739-36-2
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| Related CAS # |
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| PubChem CID |
45256693
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| Appearance |
Off-white to pink solid powder
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| LogP |
5.6
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
666
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FHWSAZXFPUMKFL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H18ClN3O3/c1-13-3-5-16(10-17(13)23(29)30)31-24-26-20-11-18(19(25)12-21(20)27-24)14-4-6-22-15(9-14)7-8-28(22)2/h3-12H,1-2H3,(H,26,27)(H,29,30)
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| Chemical Name |
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.3 mg/mL (3.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 13.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 1.3 mg/mL (3.01 mM) (saturation unknown) 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 13.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 1.3 mg/mL (3.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3155 mL | 11.5776 mL | 23.1551 mL | |
| 5 mM | 0.4631 mL | 2.3155 mL | 4.6310 mL | |
| 10 mM | 0.2316 mL | 1.1578 mL | 2.3155 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.
Effect of the small-molecule AMPK activator 991 on activity of a panel of 139 protein kinases.Am J Physiol Endocrinol Metab.2016 Oct 1;311(4):E706-E719. |
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991 treatment enhances AMPK activity induced by 5-aminoimidazole-4-carboxamide riboside (AICAR) or C13 in hepatocytes.Am J Physiol Endocrinol Metab.2016 Oct 1;311(4):E706-E719. |
991 activator binding to AMPK.Nat Commun.2013;4:3017. doi: 10.1038/ncomms4017. |
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