GW 501516 CAS 317318-70-0

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Product  NameGW501516
Synonyms2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]aceticacid;GW501516,>=98%;ENDUROBOL(GW-501516)/CARDARINE/;Cardarine(GW501516,GSK-516);GW-501615;CB646Chemicalbook5728;2-(4-((2-(4-(Trifluoromethyl)phenyl)-4-methylthiazol-5-yl)methylthio)-2-methylphenoxy)acetica;{2-Methyl-4-[4-Methyl-2-(4-trifluoroMethyl-phenyl)-thiazol-5-ylMethylsulfanyl]-phenoxy}-aceticacid
CAS NO317318-70-0
Molecular FormulaC21H18F3NO3S2
Molecular Weight453.5
Melting point 134-136C
Boiling Point584.560.0 C at 760 mmHg
Flash Point307.332.9 C
Density 1.40.1 g/cm3
Purity97%
GradePharmaceutical Grade
SolubilityDMSO: soluble20mg/mL, clear
Appearancewhite to beige powder
StorageStore at dry and cool place
Packing and ShippingPacking: Drum / Aluminum Foil  Bag / According to customer's requiement                                                      Shipping: 3-5 working days after receive payment, by  Fedex,UPS,EMS,DHL,Sea and air transport
UsageIt is the best in terms of  endurance, energy, endurance and any type of performance improvement


GW-501516 (317318-70-0) Description

GW501516 (also known as GW-501,516, GW1516, GSK-516, Cardarine,  is a PPAR receptor agonist that was invented in a collaboration between Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s. It entered into clinical development as a drug candidate for metabolic and cardiovascular diseases.

Exercise can increase peroxisome proliferator-activated receptor- (PPAR) expression in skeletal muscle. PPAR regulates muscle metabolism and reprograms muscle fibre types to enhance running endurance. This study utilized metabolomic profiling to examine the effects of GW501516, a PPAR agonist, on running endurance in mice.


GW-501516 (317318-70-0) Mechanism of Action

GW5010516 (Cardarine) binds to these PPAR receptors, which are a group of nuclear proteins found in muscles and fatty acids in the body. Hence, these receptors get activated and help the body to burn fat, increase muscle endurance, and build lean muscle. GW5010516 also has a positive effect on your vascular system.


GW-501516 (317318-70-0) Application

In rats, binding of GW501516 to PPAR recruits the coactivator PGC-1. The PPAR/coactivator complex in turn upregulates the expression of proteins involved in energy expenditure.In rats treated with GW501516, increased fatty acid metabolism in skeletal muscle and protection against diet-induced obesity and type II diabetes was observed. In obese rhesus monkeys, GW501516 increased high-density lipoprotein (HDL) and lowered very-low-density lipoprotein (VLDL).


GW-501516 (317318-70-0) Side Effects & Warning


The Danger of Using Cardarine Could Result In Brain Cell Damage

The first Cardarine animal study attempted to see if it could lower oxidative stress in the brain. The initial results were positive and showed that mice who were given Cardarine showed to have improved blood circulation in brain tissue and a lowered amount of oxidative stress.

Although the initial result looked promising, Cardarine was also discovered to have pro-inflammatory effects on the animal brain cells. For example, while Cardarine lowered certain inflammatory cytokines such as TNF (Tumor Necrosis Factor), it increased others like IL-6 (Interleukin 6), which can cause brain cell damage at elevated levels.

The study concluded the positive aspect of Cardarine on oxidative stress was quickly negated due to the high potential for brain damage.


The Danger of Using Cardarine and Liver Damage

The primary focus of studying Cardarine was how it would affect the liver. The liver is the most critical organ involved in the burning, release, and storage of fat in the body. PPAR-delta is responsible for regulating glucose metabolism and insulin sensitivity, by triggering the liver to shift its source of energy from glucose to fatty acids, thereby reducing blood sugar.

During the initial mouse and cell studies, Cardarine showed promising results as being potentially advantageous to liver health. Liver cells that were exposed to Cardarine, produced lower levels of cytokines, which was thought to aid in preventing insulin resistance. Mice who were fed a high fructose diet showed lower levels of liver damage as a result of Cardarine and had lower chances of developing fatty liver disease.


Reference

1. Koh B (2013-03-22). "Anti-doping agency warns cheats on the health risks of Endurobol". The Conversation.

2. Sahebkar A, Chew GT, Watts GF (March 2014). "New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease". Expert Opinion on Pharmacotherapy. 15 (4): 493C503. doi:10.1517/14656566.2014.876992. PMID 24428677. S2CID 21158696. Despite these promising early results, the further investigation and development of GW501516 was discontinued after observations in animal studies of its association with the rapid induction of cancers in several organs (liver, stomach, tongue, skin, bladder, ovaries, womb and testes

3. "GW501516 GlaxoSmithKline, Ligand milestone payment". R & D Focus Drug News. 28 June 2004.

4. Wolf G (November 2003). "The function of the nuclear receptor peroxisome proliferator-activated receptor delta in energy homeostasis". Nutr. Rev. 61 (11): 387C90. doi:10.1301/nr.2003.nov.387-390. PMID 14677574. S2CID 12362203.

5. Oliver WR, Shenk JL, Snaith MR, Russell CS, Plunket KD, Bodkin NL, Lewis MC, Winegar DA, Sznaidman ML, Lambert MH, Xu HE, Sternbach DD, Kliewer SA, Hansen BC, Willson TM (April 2001). "A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport". Proc. Natl. Acad. Sci. U.S.A. 98 (9): 5306C11. Bibcode:2001PNAS...98.5306O. doi:10.1073/pnas.091021198. PMC 33205. PMID 11309497.




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