| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
The primary targets of AJS1669 include glycogen synthase (GS), a key enzyme in glycogenesis, and PPARδ, a nuclear receptor involved in lipid and glucose metabolism. By activating glycogen synthase, it promotes glycogen synthesis. As a PPARδ agonist, it promotes fatty acid oxidation and improves insulin sensitivity. This dual mechanism contributes to its potential for improving glucose metabolism.
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| ln Vitro |
In vitro, AJS1669 functions as a potent activator of muscle glycogen synthase. As a PPARδ agonist, it promotes fatty acid oxidation in cells. These activities contribute to its ability to improve glucose metabolism. The compound's effects are characterized in cell-based assays measuring glycogen synthesis and gene expression of PPARδ target genes. Its potency and efficacy would be determined from dose-response studies.
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| ln Vivo |
In vivo, AJS1669 has been shown to improve glucose metabolism and reduce body fat mass in mice. Its oral availability makes it suitable for in vivo administration. By activating PPARδ, it promotes fatty acid oxidation and improves insulin sensitivity without the weight gain often associated with other PPAR agonists. These effects support its investigation for metabolic diseases.
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| Enzyme Assay |
In vitro enzyme/receptor binding studies for AJS1669 measure its activity towards glycogen synthase and PPARδ. Glycogen synthase activity can be assessed by measuring the incorporation of UDP-glucose into glycogen. PPARδ agonist activity is evaluated using cell-based reporter assays where the compound activates a PPAR response element-driven luciferase construct. Binding affinity to PPARδ can be assessed using radioligand binding or TR-FRET assays.
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| Cell Assay |
In vitro cell-based assays for AJS1669 evaluate its effects on glucose metabolism and adipogenesis. Muscle or liver cells are treated with the compound, and glucose uptake and glycogen synthesis are measured. Adipocyte differentiation can be studied in 3T3-L1 cells. The expression of PPARδ target genes involved in fatty acid oxidation is measured by qRT-PCR. Cytotoxicity is assessed to ensure safety.
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| Animal Protocol |
In vivo animal studies for AJS1669 are conducted in mouse models of metabolic disease. The compound is administered orally, and its effects on glucose metabolism are assessed by measuring blood glucose and insulin levels, and performing glucose tolerance tests. Body fat mass is measured using techniques like MRI or by weighing fat pads. Pharmacodynamic markers such as PPARδ target gene expression in tissues are analyzed.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of AJS1669 are enhanced by its free acid form, making it a valuable candidate for metabolic disease research. Its molecular weight is 513.51 g/mol. The compound is soluble in DMSO and should be stored under recommended conditions. Further PK details are available from the primary research literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of AJS1669 has not been fully published, but as a research compound, it is intended for non-human use. It is considered to have a favorable profile, as it improves insulin sensitivity without the weight gain associated with other PPAR agonists. Standard safety precautions for handling bioactive compounds should be followed.
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| Additional Infomation |
Additional information: AJS1669 is also known as AJS-1669 and AJS 1669. Its IUPAC name is 2-[[5-[[4-(4,5-difluoro-2-methylsulfanylphenyl)phenoxy]methyl]furan-2-carbonyl]-(furan-2-ylmethyl)amino]acetic acid. The product is a research tool for studying glycogen metabolism and PPARδ biology. This product is for research use only and is not approved for clinical or therapeutic applications.
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| Molecular Formula |
C26H20F2NNAO6S
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|---|---|
| Molecular Weight |
535.491683959961
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| Exact Mass |
513.105
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| CAS # |
1853130-05-8
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| Related CAS # |
1853130-05-8 (free acid);
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| PubChem CID |
91809198
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| Appearance |
White to off-white solid powder
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| LogP |
4.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
36
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| Complexity |
739
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CSC1=CC(=C(C=C1C2=CC=C(C=C2)OCC3=CC=C(O3)C(=O)N(CC4=CC=CO4)CC(=O)O)F)F
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| InChi Key |
IQZYODALPHIPRX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H21F2NO6S/c1-36-24-12-22(28)21(27)11-20(24)16-4-6-17(7-5-16)34-15-19-8-9-23(35-19)26(32)29(14-25(30)31)13-18-3-2-10-33-18/h2-12H,13-15H2,1H3,(H,30,31)
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| Chemical Name |
2-[[5-[[4-(4,5-difluoro-2-methylsulfanylphenyl)phenoxy]methyl]furan-2-carbonyl]-(furan-2-ylmethyl)amino]acetic acid
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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 : ~250 mg/mL (~486.85 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.05 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 20.8 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: ≥ 2.08 mg/mL (4.05 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 | 1.8674 mL | 9.3372 mL | 18.6745 mL | |
| 5 mM | 0.3735 mL | 1.8674 mL | 3.7349 mL | |
| 10 mM | 0.1867 mL | 0.9337 mL | 1.8674 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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