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GW0742, also known as GW610742, is an effective selective agonist of the synthetic peroxisome proliferator-activated receptor β/δ (PPARβ/δ). Its CAS number is 317318-84-6, the molecular formula is C21H17F4NO3S2, and the molecular weight is 471.49. From the appearance, this product is usually a solid powder ranging from white to light yellow. In terms of solubility, it has a relatively high solubility in DMSO (dimethyl sulfoxide), such as ≥34 mg/mL (72.11 mM) in DMSO, but is almost insoluble in water. When storing, it is generally recommended to keep it at -20° C. The powder form can be stably stored for 2 years. If dissolved in a solvent and stored at -80°C, the validity period is 2 years. If stored at -20°C, it should be used within 1 month as much as possible.
This product was originally developed by GlaxoSmithKline and it is an analogue of GW501516. As a selective peroxisome proliferator-activated receptor δ (PPARδ) agonist, its development aims to explore its potential applications in regulating metabolism, inflammation, etc. With the in-depth study of the function of the PPARδ receptor, scientists have discovered that PPARδ plays an important role in multiple physiological processes such as energy metabolism, lipid metabolism, and inflammatory response. Therefore, the development of agonists targeting this receptor has significant scientific significance and potential application value.
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GW0742 powder COA
Basic Information
This powder is an effective selective agonist for the synthesis of peroxisome proliferator-activated receptor β/δ (PPARβ/δ).Its CAS number is 317318-84-6, the molecular formula is C21H17F4NO3S2, and the molecular weight is 471.49. This compound has a specific chemical structure. Its full English name is 2-[4-[[2-[3-fluoro-4-(trifluoromethyl)phenyl]-4-methyl-1,3-thiazol-5-yl]methylsulfanyl]-2-methylphenoxy]acetic acid.
Physical Properties
Appearance and condition: GW0742 usually appears as a solid powder ranging from white to light yellow.
Density: approximately 1.462g/cm³.
Boiling point: At 760 mmHg, the boiling point is approximately 591.476°C.
Flash point: Approximately 311.514°C.
Refractive index: approximately 1.609.
Solubility: It has a relatively high solubility in DMSO (dimethyl sulfoxide), usually greater than 5 mg/mL, but is almost insoluble in water.
Chemical Stability and Storage Conditions
It is relatively stable under appropriate storage conditions. However, its stability may be affected by environmental factors such as temperature, light and humidity.
To maintain the stability and activity of this powder, it is recommended to store it in a low-temperature environment of -20℃, away from light and moisture. The validity period of the powder can reach up to 2 years.If dissolved in a solvent, it is recommended to store it at -80°C and use it within 6 months. If stored at -20°C, it is recommended to use it within one month as much as possible.
Chemical Activity and Selectivity
PPARβ/δ agonist
This product is a highly selective PPARβ/δ agonist. It can specifically bind to the PPARβ/δ receptor, activate the receptor and cause conformational changes in it, and then recruit coactivators to form transcriptional complexes.
Selectivity
Its selectivity for PPARβ/δ is much higher than that for PPARα and PPARγ. Among them, the EC50 values of this powder for human PPARδ, PPARα and PPARγ are 1 nM, 1.1 μM and 2 μM respectively, and it has a high selectivity for PPARδ.
Chemical Reactivity
Although the specific chemical reactivity of this product varies depending on the experimental conditions, as an organic compound, it can participate in various chemical reactions, such as substitution reactions and addition reactions. However, under normal storage and usage conditions, it has high chemical stability and is not prone to spontaneous reactions.
GW0742 (GW610742) is a highly selective peroxisome proliferator-activated receptor β/δ (PPARβ/δ) agonist and plays a key role in multiple physiological and pathological processes. The following will elaborate in detail on the functions of this product in metabolic regulation, anti-inflammation, neuroprotection, joint health promotion and other potential therapeutic fields.
Metabolic regulatory function
This product significantly enhances exercise endurance by activating the PPARβ/δ receptor. It can increase the number and density of mitochondria in muscle tissue. As the "energy factory" of cells, mitochondria enhance metabolic efficiency, enabling the body to produce more ATP during exercise and providing sufficient energy for muscle contraction. This effect not only extends the maximum duration of aerobic exercise but also enhances the muscles' resistance to fatigue, enabling athletes to withstand greater training intensifies. In addition, it can also accelerate the recovery process of the body after exercise. By regulating the expression of genes related to muscle repair and regeneration, it reduces fatigue and muscle soreness after exercise, enabling athletes to recover to their best condition more quickly for the next training session.
This product performs exceptionally well in lipid metabolism regulation. It can enhance the oxidation of fatty acids, increase the density of mitochondria in cells, and enable the body to utilize fat as an energy source more effectively. By converting the fat stored in cells and the fat in daily diet into fuel for muscles, this product can accelerate the breakdown and metabolism of fat, significantly reducing body fat content, especially in areas prone to fat accumulation such as the waist. Meanwhile, it can also increase muscle mass. By stimulating the expression of anti-inflammatory cytokines IL-10 and TGF-β mRNA, it enhances the rate of myogenesis, enabling muscles to regenerate and repair more quickly after injury. This effect of reducing fat without losing muscle makes it have potential application value in the fields of fitness and fat loss.
This product can also improve insulin sensitivity and is of great significance for the prevention and treatment of metabolic diseases such as diabetes. By activating the PPARβ/δ receptor, this product can regulate the expression of genes related to glucose metabolism, promote the uptake and utilization of glucose, and thereby reduce blood sugar levels. This effect not only helps to improve the symptoms of diabetic patients, but may also delay the occurrence and development of diabetic complications.
Anti-inflammatory function
Inhibit the expression of inflammatory cytokines
GW0742 has a significant anti-inflammatory effect and can inhibit the expression of various pro-inflammatory cytokines. In the LPS-mediated pulmonary inflammation model, this product significantly reduced the protein and mRNA levels of pro-inflammatory cytokines IL-6, IL-1β and TNF-α. These cytokines play a key role in the inflammatory response. Their reduction helps to alleviate the degree of the inflammatory response and improve the symptoms of inflammatory diseases.
Regulate inflammatory signaling pathways
This product exerts anti-inflammatory effects by regulating inflammatory signaling pathways. It can block the increase of IL-1β mRNA and ERK phosphorylation in radiation-induced brain injury, thereby reducing the damage of inflammation to tissues. Furthermore, it can also prevent bleomycin-induced degradation of IkB-a, reduce the level of NF-kB p65 in the lungs, and decrease the expression of iNOS and p-ERK in bleomycin-induced mice. These effects indicate that it plays a regulatory role in multiple links of the inflammatory signaling pathway, providing new molecular targets for the treatment of inflammatory diseases.
The application potential in various inflammatory diseases
Based on its anti-inflammatory properties, this product has shown potential application value in the treatment of various inflammatory diseases. For example, in inflammatory diseases such as autoimmune diseases, chronic obstructive pulmonary disease (COPD), and atherosclerosis, it may improve disease symptoms by inhibiting inflammatory responses and reducing tissue damage. In addition, this product can also be used in combination with existing anti-inflammatory drugs to enhance the therapeutic effect, reduce the dosage and side effects of the drugs.
Neuroprotective function
Reduce nerve cell damage
This product has a protective effect on nerve cells and can reduce the damage and death of nerve cells. In neurodegenerative disease models, it reduces neuronal apoptosis and necrosis by activating the PPARβ/δ receptor and regulating the expression of genes related to the survival and apoptosis of nerve cells. This effect helps to delay the progression of neurodegenerative diseases and protect the function of the nervous system.
Improve neurological function
In addition to reducing nerve cell damage, this product can also improve nerve function. It can promote the formation and remodeling of neural synapses and enhance the connection and conduction efficiency of neural networks. In the neural injury model, this product can accelerate the recovery of neural function and improve the cognitive and behavioral abilities of animals. These functions indicate that it has potential application value in neuroprotection and repair.
Joint health promotion function
Strengthen cartilage formation and repair
This product plays an important role in promoting joint health. It can promote the chondrogenic differentiation of human synovial fluid-derived mesenchymal stem cells (HSV-Mscs), and increase the proliferation and differentiation ability of chondrocytes. By activating the PPARβ/δ receptor, this product regulates the expression of genes related to cartilage formation and repair, promoting the synthesis and deposition of cartilage matrix. This effect helps prevent joint degeneration, repair damaged cartilage tissue and improve joint function.
Relieve joint inflammation and pain
In addition to promoting cartilage formation and repair, this product can also alleviate joint inflammation and pain. It can inhibit the expression of pro-inflammatory cytokines in the synovial membrane of joints and reduce the infiltration and activation of inflammatory cells. Meanwhile, this product can also promote the production of anti-inflammatory cytokines, regulate the immune microenvironment of joints, and alleviate joint inflammation and pain. These functions make this product have potential application value in the treatment of joint diseases such as osteoarthritis.
The potential of combined treatment for osteoarthritis
Studies have shown that this product combined with HSC-Mscs in the treatment of osteoarthritis may have a better effect. Hsv-mscs have multi-directional differentiation potential and immunomodulatory functions, and can promote cartilage repair and reduce inflammation. This product can enhance the chondrogenic differentiation ability and anti-inflammatory effect of HSV-Mscs. The combined use of the two may produce a synergistic effect and improve the therapeutic effect. This discovery provides new ideas and methods for the treatment of osteoarthritis.
Other potential therapeutic functions
Cardiovascular protection
This product also shows potential in cardiovascular protection. It can regulate lipid metabolism and energy metabolism, lower blood lipid levels, and reduce the risk of atherosclerosis. Meanwhile, this product can also inhibit the proliferation and migration of vascular smooth muscle cells, and alleviate vascular inflammation and damage. These functions help protect the health of the cardiovascular system and prevent the occurrence of cardiovascular diseases.
Anti-tumor effect
Recent studies have shown that this product may have certain anti-tumor effects. It can inhibit the proliferation and invasion ability of tumor cells by regulating their metabolism and signaling pathways. Meanwhile, this product can also enhance the immune function of the body and promote the apoptosis and clearance of tumor cells. However, at present, there are relatively few studies on its anti-tumor effect, and further experiments and clinical studies are needed to verify its efficacy and safety.
Other potential applications
In addition to the above functions, this product may also have potential application value in other fields. For instance, in the treatment of metabolic diseases such as metabolic syndrome, obesity and diabetes, GW0742 may improve disease symptoms by regulating lipid metabolism and energy metabolism. In addition, in fields such as neurological diseases and immune system diseases, this product may also play a certain therapeutic role.
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