CARDARINE (GW-501516) – Solution, 600mg (20mg/mL)

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Cardarine GW-501516


GW-501516 is a PPAR (peroxisome proliferator-activated receptor) agonist originally developed for hyperlipidemia, obesity, metabolic dysfunction and heart disease by GlaxoSmithKline, a multinational pharmaceutical company.


The compound is also known by other names Endoburol, Cardarine, and is commonly used in research studies, cited as a PPARδ agonist.


Several studies have shown that GW-501516 affects fatty acid metabolism, skeletal muscle endurance and glucose/insulin balance.


Since PPARδ plays an important role in mitochondrial respiration, temperature regulation, inflammatory mediation, skin and muscle repair, skeletal reprogramming, and keratinocyte differentiation, it can be assumed that GW501516 may have an impact on these additional areas. https://academic.oup.com/endo/article/151/4/1560/2456696 ? login=true


One mouse study clearly demonstrates the impact of GW5015016 on mouse endurance, both in trained and untrained mice.


After three weeks of GW-501516, trained rats showed a 31.2 percent increase in their total walking distance, while untrained rats increased their total distance by 68.6 percent. Even one week of GW5015016 increased walking distance by 48.6 percent over the control group.


In the group that both received Cardarine and had previously been trained to run, higher use of longer saturated fatty acids, as well as triglycerides, was found to improve endurance, probably due to increased fatty acid metabolism after PPARδ activation, inhibiting PDK4 and other mediating pathways. of fatty acid oxidation. (https://www.nature.com/articles/srep09884?post=06172017a)_


Molecular analyzes revealed that PPARδ is involved in exercise-induced muscle fiber reprogramming and skeletal muscle metabolism by regulating the expression of genes associated with contractile proteins, mitochondrial biogenesis and lipid oxidation.


Another study confirmed the above by administering GW501516 to mice fed a high-fat diet. The dosed group experienced only slight weight loss, but metabolic markers such as decreased insulin resistance, increased metabolism, increased mitochondria and decreased lipids in skeletal muscle were noted. In addition, plasma glucose and blood insulin were reduced in genetically obese mice.


https://www.pnas.org/content/100/26/15924.short

One study indicated that GW-501516 may also play a role in reducing inflammation, particularly in the liver. For rats fed a high fructose diet, GW-501516 reduced the ACE/AT1r axis inflammatory markers. In addition, it increased the genes that regulate beta oxidation and decreased the genes that regulate the production of fat cells and glucose. ( https://link.springer.com/article/10.1007/s12020-015- 0590-1 )


Similar results were noted in primate studies, a study of middle-aged overweight to obese rhesus monkeys indicated that HDL cholesterol was elevated, LDL was decreased, along with fasting triglycerides and fasting insulin levels. Researchers believed that GW501516 could be a major breakthrough for cardiovascular diseases such as atherosclerosis and reduce the severity of metabolic syndromes. https://www.pnas.org/content/ 98/9/5306.short



Concentration

20mg/ml.


DISCLAIMER

This material is sold for use in laboratory research only. Terms of sale apply. Not for human consumption, nor for medical, veterinary or domestic use. Please familiarize yourself with our DISCLAIMER before ordering.

Data Sheet

Cardarine (GW501516) – Solution, 600mg (20mg/mL)

Application PPARδ receptor agonist
CAS 317318-70-0
Molar Mass 453.498 g/mol
 Chemical Formula C21H18F3NO3S2
IUPAC Name {4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]-2-methylphenoxy}acetic acid
Synonyms GW501516, Cardarine, Endurobol, GSK-516
Storage Room temperature
Solubility Soluble in Ethanol, PEG400
Organoleptic Profile Clear Liquid
Physical Form Solution in PEG400
Specification 20mg/mL ±5%
Terms This material is sold for laboratory research use only. Terms of sale apply. Not for human consumption, nor medical, veterinary, or household uses. Please familiarize yourself with our Terms & Conditions prior to ordering.
Additional Notes This compound was withdrawn from clinical trials due to promotion of carcinogenesis.

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