| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg | |||
| Other Sizes |
| Targets |
AMP-activated protein kinase (AMPK).
|
|---|---|
| ln Vitro |
Ampkinone promotes AMPK phosphorylation via indirectly activating AMPK in numerous cell lines. Ampkinone-mediated activation of AMPK requires the activity of LKB1 and leads to enhanced glucose uptake in muscle cells [1].
Ampkinone is an indirect AMPK activator. It stimulates AMPK phosphorylation at Thr172 through an LKB1-dependent mechanism, leading to enhanced glucose uptake in muscle cells with an EC50 of 4.3 uM. This activation occurs indirectly in several cell lines. |
| ln Vivo |
Mice treated with ampkinone showed a considerable reduction in both total body weight and total fat mass. The DIO mice model's metabolic problems can be significantly improved by Ampkinone, according to histological inspection and blood lipid parameter assessment [1].
Ampkinone-mediated activation of AMPK leads to enhanced glucose uptake in muscle cells. In vivo, it is expected to improve glucose metabolism and insulin sensitivity, with potential benefits in obesity and type 2 diabetes. |
| Enzyme Assay |
AMPK kinase activity assays are performed using purified recombinant AMPK. The compound is incubated with AMPK and ATP. Phosphorylation of AMPK or a peptide substrate is measured using radioactive or fluorescence-based methods.
|
| Cell Assay |
Muscle cells (e.g., L6 myotubes) are treated with Ampkinone. AMPK phosphorylation (p-AMPK Thr172) is measured by Western blot. Glucose uptake is assessed using radiolabeled 2-deoxyglucose. The requirement for LKB1 is confirmed using LKB1-deficient cells.
|
| Animal Protocol |
Animal models of obesity and type 2 diabetes (e.g., high-fat diet-fed mice or db/db mice) are used to assess the in vivo efficacy of Ampkinone. Glucose tolerance tests, insulin sensitivity, and metabolic parameters are measured following chronic treatment.
|
| ADME/Pharmacokinetics |
Predicted to have moderate oral bioavailability. The compound's lipophilic nature suggests good tissue penetration. Metabolism is likely mediated by CYP450 enzymes. Half-life in rodents is estimated to be 2-4 hours.
|
| Toxicity/Toxicokinetics |
No specific toxicity data reported for Ampkinone. AMPK activators are generally well-tolerated in preclinical studies. No significant genotoxicity or cardiotoxicity concerns have been reported.
|
| References | |
| Additional Infomation |
Ampkinone is an organic heterotetracyclic compound with the structure [1] benzopyrano[3,4-e]isoindole-1,3(2H,4H)-dione, substituted at positions 2, 4, 4, 6, and 7 with 4-benzoylphenyl, methyl, hydroxyl, and methoxy, respectively. It is an indirect small-molecule activator of AMPK and a potential drug for the treatment of obesity and type 2 diabetes. It has hypoglycemic, protein kinase agonist, and anti-obesity effects. It belongs to the benzophenone class of compounds, is an ether compound, and is also an organic heterotetracyclic compound.
Ampkinone is a research tool for studying AMPK-mediated signaling and the therapeutic potential of AMPK activation in metabolic diseases. It has not been approved for clinical use. The compound's mechanism involves indirect activation of AMPK through the LKB1 pathway, leading to improved glucose metabolism. |
| Molecular Formula |
C31H23NO6
|
|---|---|
| Molecular Weight |
505.51742
|
| Exact Mass |
505.152
|
| CAS # |
1233082-79-5
|
| PubChem CID |
49843507
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.4±0.1 g/cm3
|
| Boiling Point |
732.7±70.0 °C at 760 mmHg
|
| Flash Point |
396.9±35.7 °C
|
| Vapour Pressure |
0.0±2.5 mmHg at 25°C
|
| Index of Refraction |
1.666
|
| LogP |
4.7
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
38
|
| Complexity |
935
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC1(C2=C(C=CC3=C2C(=O)N(C3=O)C4=CC=C(C=C4)C(=O)C5=CC=CC=C5)C6=C(O1)C(=C(C=C6)OC)O)C
|
| InChi Key |
BRRCHDIWBKOMEC-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C31H23NO6/c1-31(2)25-20(21-15-16-23(37-3)27(34)28(21)38-31)13-14-22-24(25)30(36)32(29(22)35)19-11-9-18(10-12-19)26(33)17-7-5-4-6-8-17/h4-16,34H,1-3H3
|
| Chemical Name |
2-(4-benzoylphenyl)-6-hydroxy-7-methoxy-4,4-dimethylchromeno[3,4-e]isoindole-1,3-dione
|
| 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 (In Vitro) |
DMSO : ~50 mg/mL (~98.91 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.95 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9782 mL | 9.8908 mL | 19.7816 mL | |
| 5 mM | 0.3956 mL | 1.9782 mL | 3.9563 mL | |
| 10 mM | 0.1978 mL | 0.9891 mL | 1.9782 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
