| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
GLUT4 (glucose transporter type 4). This compound activates GLUT4 translocation, a process by which GLUT4 vesicles are mobilized from intracellular compartments to the cell surface in response to insulin signaling. By promoting GLUT4 membrane trafficking, the compound enhances glucose uptake in insulin-sensitive tissues such as skeletal muscle and adipose tissue.
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| ln Vitro |
GLUT4 activator 1 shows potent in vitro activity with an EC₅0 of 0.14 microM for promoting GLUT4 translocation. The compound is assessed in cell-based assays measuring GLUT4-GFP translocation to the plasma membrane upon compound treatment. Its efficacy is demonstrated by increased cell surface GLUT4 levels and enhanced glucose uptake in cultured adipocytes or muscle cells.
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| ln Vivo |
In vivo, GLUT4 activator 1 exhibits hypoglycemic effects, lowering blood glucose levels in animal models. As an orally active compound, it is suitable for oral administration in preclinical studies. Efficacy would be demonstrated in diabetic rodent models (e.g., db/db mice or STZ-induced diabetic rats) by measuring reductions in fasting blood glucose and improvements in glucose tolerance.
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| Enzyme Assay |
In vitro GLUT4 translocation assays typically use 3T3-L1 adipocytes or L6 myotubes stably expressing GLUT4-GFP or GLUT4-myc. Cells are serum-starved, then treated with serial dilutions of test compound. Translocation is quantified by fluorescence microscopy (GFP redistribution to the plasma membrane) or by measuring cell surface myc-tag antibody binding. EC₅0 values are calculated from dose-response curves.
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| Cell Assay |
3T3-L1 adipocytes differentiated from preadipocytes are seeded in 96-well plates and transfected or transduced with GLUT4-GFP. After serum starvation, cells are treated with compound for 30-60 minutes. Cells are fixed and imaged, and the plasma membrane-to-cytoplasm fluorescence ratio is quantified using high-content imaging systems. Alternatively, 2-deoxyglucose uptake assays measure functional glucose transport.
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| Animal Protocol |
Diabetic rodent models (db/db mice or high-fat diet-fed mice) are administered GLUT4 activator 1 orally at various doses. Blood glucose levels are measured at baseline and at multiple time points post-administration. Oral glucose tolerance tests (OGTT) are performed to assess glucose disposal. Insulin levels may also be measured to determine whether the compound acts independently of insulin.
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| ADME/Pharmacokinetics |
GLUT4 activator 1 has a molecular weight of 452.5 g/mol and formula C23H21FN4O3S. As an orally active compound, it is expected to have favorable oral bioavailability. Standard PK studies in rodents would determine parameters such as half-life, Cmax, Tmax, AUC, and oral bioavailability following PO and IV administration. The compound is formulated in suitable vehicles for oral gavage.
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| Toxicity/Toxicokinetics |
Toxicology data for GLUT4 activator 1 are not publicly available. Standard preclinical safety assessment would include cytotoxicity assays, hERG channel inhibition testing, and repeat-dose toxicology studies in rodents to identify potential target organs and determine the no-observed-adverse-effect level (NOAEL).
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| References | |
| Additional Infomation |
GLUT4 activator 1 is a research compound for diabetes and metabolic disease studies. It is not approved for clinical use. The compound is useful for studying GLUT4 trafficking mechanisms and identifying novel insulin-independent pathways for glucose uptake. It may serve as a lead compound for developing new antidiabetic agents that bypass insulin resistance.
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| Molecular Formula |
C23H21FN4O3S
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|---|---|
| Molecular Weight |
452.50
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| Exact Mass |
452.131
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| CAS # |
2253733-37-6
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| PubChem CID |
138454789
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| Appearance |
White to light yellow solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
32
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| Complexity |
618
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(CC(N)=O)=CC=C(NC2=NN=C(C3=CC=CC=C3OCCOC)C3SC=CC=32)C(F)=C1
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| InChi Key |
GWLCNGUGZNFYHI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H21FN4O3S/c1-30-9-10-31-19-5-3-2-4-15(19)21-22-16(8-11-32-22)23(28-27-21)26-18-7-6-14(12-17(18)24)13-20(25)29/h2-8,11-12H,9-10,13H2,1H3,(H2,25,29)(H,26,28)
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| Chemical Name |
2-[3-fluoro-4-[[7-[2-(2-methoxyethoxy)phenyl]thieno[2,3-d]pyridazin-4-yl]amino]phenyl]acetamide
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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 |
| 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) |
DMSO : ~100 mg/mL (~220.99 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.52 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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.52 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (5.52 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2099 mL | 11.0497 mL | 22.0994 mL | |
| 5 mM | 0.4420 mL | 2.2099 mL | 4.4199 mL | |
| 10 mM | 0.2210 mL | 1.1050 mL | 2.2099 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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