juced_porkchop
Moderator
We are now carring a Brand new compound at uniquemicals.com and wanted to post up some info on this for those unaware of its use. 
GW-501516 (also known as GW-501,516,GW1516 or GSK-516) is a PPAR***948; modulator compound being investigated for drug use by GlaxoSmithKline.[1][2] It activates the same pathways activated through exercise, including PPAR***948; and AMP-activated protein kinase. It is being investigated as a potential treatment for obesity, diabetes, dyslipidemia and cardiovascular disease. [3] [4] GW-501516 has a synergistic effect when combined with AICAR: the combination has been shown to significantly increase exercise endurance in animal studies more than either compound alone. [5][6]
GW-50156 regulates fat burning through a number of widespread mechanisms [7]; it increases glucose uptake in skeletal muscle tissue and increases muscle gene expression, especially genes involved in preferential lipid utilization.,[8][9] [10] This shift changes the body's metabolism to favor burning fat for energy instead of carbohydrates or muscle protein, potentially allowing clinical application for obese patients to lose fat effectively without experiencing muscle catabolism or the effects and satiety issues associated with low blood sugar. [11] GW-501516 also increases muscle mass, which improved glucose tolerance and reduced fat mass accumulation even in mice fed a very high fat diet, suggesting that GW-501516 may have a protective effect against obesity [12]
It has been demonstrated at oral doses of 5 mg a day to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome, most likely by stimulating fatty acid oxidation.[13] Treatments with GW-501516 have been shown to increase HDL cholesterol by up to 79% in rhesus monkeys and the compound is now undergoing Phase II trials to improve HDL cholesterol in humans. [14]
Concerns were raised prior to the 2008 Beijing Olympics that GW-501516 could be used by athletes as a performance enhancing drug which was not currently controlled by regulations or detected by standard tests. One of the main researchers from the study on enhanced endurance consequently developed a urine test to detect the drug, and made it available to the International Olympic Committee.[15] The World Anti-Doping Agency has also begun work on a test GW-501516 and other related PPAR***948; modulators.,[16] and they have been added to the prohibited list from 2009 onwards.[17] The compound has yet to be named a controlled or prohibited substance by any nation's drug enforcement or regulation agency. To date, no athlete is known to have tested positive for the substance, though the increase in endurance, muscle fiber performance, fat loss and metabolism suggests GW-501516 has the potential for ergogenic use and abuse.
References
^ Sznaidman ML, Haffner CD, Maloney PR, Fivush A, Chao E, Goreham D, Sierra ML, LeGrumelec C, Xu HE, Montana VG, Lambert MH, Willson TM, Oliver WR Jr, Sternbach DD (May 2003). "Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity". Bioorg. Med. Chem. Lett. 13 (9): 1517–21. doi:10.1016/S0960-894X(03)00207-5. PMID 12699745.
^ Dimopoulos N, Watson M, Green C, Hundal HS (October 2007). "The PPARdelta agonist, GW501516, promotes fatty acid oxidation but has no direct effect on glucose utilisation or insulin sensitivity in rat L6 skeletal muscle cells". FEBS Lett. 581 (24): 4743–8. doi:10.1016/j.febslet.2007.08.072. PMID 17869249.
^ Barish GD, Narkar VA, Evans RM (March 2006). "PPAR delta: a dagger in the heart of the metabolic syndrome". J. Clin. Invest. 116 (3): 590–7. doi:10.1172/JCI27955. PMC 1386117. PMID 16511591.
^
Uwe Dressel,
Tamara L. Allen,
Jyotsna B. Pippal,
Paul R. Rohde,
Patrick Lau,
and George E. O. Musc
at (2003 doi=doi:10.1210/me.2003-015). [The Peroxisome Proliferator-Activated Receptor "The Peroxisome Proliferator-Activated Receptor ***946;/***948; Agonist, GW501516, Regulates the Expression of Genes Involved in Lipid Catabolism and Energy Uncoupling in Skeletal Muscle Cells"]. Molecular Endocrinology (17): 2477-93.
^ Narkar VA, Downes M, Yu RT, Embler E, Wang Y-X, Banayo E, Mihaylova MM, Nelson MC, Zou Y, Juguilon H, Kang H, Shaw RJ,2 Evans RM (August 2008). "AMPK and PPAR***948; Agonists Are Exercise Mimetics" (PDF). Cell 134 (3): 1–11. doi:10.1016/j.cell.2008.06.051. PMC 2706130. PMID 18674809.
^ "Exercise In A Pill: Researchers Identify Drugs That Enhance Exercise Endurance". Science News. ScienceDaily. 2008-08-01. Retrieved 2008-08-01.
^ Normal 0 false false false EN-US X-NONE X-NONE ScienceDirect - Cell : Peroxisome-Proliferator-Activated Receptor ? Activates Fat Metabolism to Prevent Obesity
^ Vihang A. Narkar, Michael Downes, Ruth T. Yu, Emi Embler, Yong-Xu Wang, Ester Banayo, Maria M. Mihaylova, Michael C. Nelson, Yuhua Zou, Henry Juguilon, Heonjoong Kang, Reuben J. Shaw, Ronald M. Evans, AMPK and PPAR***948; Agonists Are Exercise Mimetics, Cell, Volume 134, Issue 3, 8 August 2008, Pages 405-415, ISSN 0092-8674, 10.1016/j.cell.2008.06.051. (http://www.sciencedirect.com/science/article/pii/S0092867408008386)}}
^ Krämer DK, Al-Khalili L, Guigas B, Leng Y, Garcia-Roves PM, Krook A (July 2007). "Role of AMP kinase and PPARdelta in the regulation of lipid and glucose metabolism in human skeletal muscle". J. Biol. Chem. 282 (27): 19313–20. doi:10.1074/jbc.M702329200. PMID 17500064.
^ Normal 0 false false false EN-US X-NONE X-NONE The Peroxisome Proliferator-Activated Receptor
^ The Peroxisome Proliferator-Activated Receptor
^ Normal 0 false false false EN-US X-NONE X-NONE PLoS Biology: Regulation of Muscle Fiber Type and Running Endurance by PPAR
^ Risérus U, Sprecher D, Johnson T, Olson E, Hirschberg S, Liu A, Fang Z, Hegde P, Richards D, Sarov-Blat L, Strum JC, Basu S, Cheeseman J, Fielding BA, Humphreys SM, Danoff T, Moore NR, Murgatroyd P, O'Rahilly S, Sutton P, Willson T, Hassall D, Frayn KN, Karpe F (February 2008). "Activation of peroxisome proliferator-activated receptor (PPAR)delta promotes reversal of multiple metabolic abnormalities, reduces oxidative stress, and increases fatty acid oxidation in moderately obese men". Diabetes 57 (2): 332–9. doi:10.2337/db07-1318. PMID 18024853.
^ Normal 0 false false false EN-US X-NONE X-NONE GW-501516 GlaxoSmithKline/Ligand
^ "AICAR and GW 1516 - The Exercise Pill". Retrieved 2008-09-18.
^ Laurance J, Rajan A (2008-08-01). "Warning to Beijing Olympics over pills that mimic exercise". Health News, Health & Wellbeing. The Independent. Retrieved 2008-08-01.
^ WADA 2009 Prohibited List
GW-501516 (also known as GW-501,516,GW1516 or GSK-516) is a PPAR***948; modulator compound being investigated for drug use by GlaxoSmithKline.[1][2] It activates the same pathways activated through exercise, including PPAR***948; and AMP-activated protein kinase. It is being investigated as a potential treatment for obesity, diabetes, dyslipidemia and cardiovascular disease. [3] [4] GW-501516 has a synergistic effect when combined with AICAR: the combination has been shown to significantly increase exercise endurance in animal studies more than either compound alone. [5][6]
GW-50156 regulates fat burning through a number of widespread mechanisms [7]; it increases glucose uptake in skeletal muscle tissue and increases muscle gene expression, especially genes involved in preferential lipid utilization.,[8][9] [10] This shift changes the body's metabolism to favor burning fat for energy instead of carbohydrates or muscle protein, potentially allowing clinical application for obese patients to lose fat effectively without experiencing muscle catabolism or the effects and satiety issues associated with low blood sugar. [11] GW-501516 also increases muscle mass, which improved glucose tolerance and reduced fat mass accumulation even in mice fed a very high fat diet, suggesting that GW-501516 may have a protective effect against obesity [12]
It has been demonstrated at oral doses of 5 mg a day to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome, most likely by stimulating fatty acid oxidation.[13] Treatments with GW-501516 have been shown to increase HDL cholesterol by up to 79% in rhesus monkeys and the compound is now undergoing Phase II trials to improve HDL cholesterol in humans. [14]
Concerns were raised prior to the 2008 Beijing Olympics that GW-501516 could be used by athletes as a performance enhancing drug which was not currently controlled by regulations or detected by standard tests. One of the main researchers from the study on enhanced endurance consequently developed a urine test to detect the drug, and made it available to the International Olympic Committee.[15] The World Anti-Doping Agency has also begun work on a test GW-501516 and other related PPAR***948; modulators.,[16] and they have been added to the prohibited list from 2009 onwards.[17] The compound has yet to be named a controlled or prohibited substance by any nation's drug enforcement or regulation agency. To date, no athlete is known to have tested positive for the substance, though the increase in endurance, muscle fiber performance, fat loss and metabolism suggests GW-501516 has the potential for ergogenic use and abuse.
References
^ Sznaidman ML, Haffner CD, Maloney PR, Fivush A, Chao E, Goreham D, Sierra ML, LeGrumelec C, Xu HE, Montana VG, Lambert MH, Willson TM, Oliver WR Jr, Sternbach DD (May 2003). "Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)--synthesis and biological activity". Bioorg. Med. Chem. Lett. 13 (9): 1517–21. doi:10.1016/S0960-894X(03)00207-5. PMID 12699745.
^ Dimopoulos N, Watson M, Green C, Hundal HS (October 2007). "The PPARdelta agonist, GW501516, promotes fatty acid oxidation but has no direct effect on glucose utilisation or insulin sensitivity in rat L6 skeletal muscle cells". FEBS Lett. 581 (24): 4743–8. doi:10.1016/j.febslet.2007.08.072. PMID 17869249.
^ Barish GD, Narkar VA, Evans RM (March 2006). "PPAR delta: a dagger in the heart of the metabolic syndrome". J. Clin. Invest. 116 (3): 590–7. doi:10.1172/JCI27955. PMC 1386117. PMID 16511591.
^
Uwe Dressel,
Tamara L. Allen,
Jyotsna B. Pippal,
Paul R. Rohde,
Patrick Lau,
and George E. O. Musc
at (2003 doi=doi:10.1210/me.2003-015). [The Peroxisome Proliferator-Activated Receptor "The Peroxisome Proliferator-Activated Receptor ***946;/***948; Agonist, GW501516, Regulates the Expression of Genes Involved in Lipid Catabolism and Energy Uncoupling in Skeletal Muscle Cells"]. Molecular Endocrinology (17): 2477-93.
^ Narkar VA, Downes M, Yu RT, Embler E, Wang Y-X, Banayo E, Mihaylova MM, Nelson MC, Zou Y, Juguilon H, Kang H, Shaw RJ,2 Evans RM (August 2008). "AMPK and PPAR***948; Agonists Are Exercise Mimetics" (PDF). Cell 134 (3): 1–11. doi:10.1016/j.cell.2008.06.051. PMC 2706130. PMID 18674809.
^ "Exercise In A Pill: Researchers Identify Drugs That Enhance Exercise Endurance". Science News. ScienceDaily. 2008-08-01. Retrieved 2008-08-01.
^ Normal 0 false false false EN-US X-NONE X-NONE ScienceDirect - Cell : Peroxisome-Proliferator-Activated Receptor ? Activates Fat Metabolism to Prevent Obesity
^ Vihang A. Narkar, Michael Downes, Ruth T. Yu, Emi Embler, Yong-Xu Wang, Ester Banayo, Maria M. Mihaylova, Michael C. Nelson, Yuhua Zou, Henry Juguilon, Heonjoong Kang, Reuben J. Shaw, Ronald M. Evans, AMPK and PPAR***948; Agonists Are Exercise Mimetics, Cell, Volume 134, Issue 3, 8 August 2008, Pages 405-415, ISSN 0092-8674, 10.1016/j.cell.2008.06.051. (http://www.sciencedirect.com/science/article/pii/S0092867408008386)}}
^ Krämer DK, Al-Khalili L, Guigas B, Leng Y, Garcia-Roves PM, Krook A (July 2007). "Role of AMP kinase and PPARdelta in the regulation of lipid and glucose metabolism in human skeletal muscle". J. Biol. Chem. 282 (27): 19313–20. doi:10.1074/jbc.M702329200. PMID 17500064.
^ Normal 0 false false false EN-US X-NONE X-NONE The Peroxisome Proliferator-Activated Receptor
^ The Peroxisome Proliferator-Activated Receptor
^ Normal 0 false false false EN-US X-NONE X-NONE PLoS Biology: Regulation of Muscle Fiber Type and Running Endurance by PPAR
^ Risérus U, Sprecher D, Johnson T, Olson E, Hirschberg S, Liu A, Fang Z, Hegde P, Richards D, Sarov-Blat L, Strum JC, Basu S, Cheeseman J, Fielding BA, Humphreys SM, Danoff T, Moore NR, Murgatroyd P, O'Rahilly S, Sutton P, Willson T, Hassall D, Frayn KN, Karpe F (February 2008). "Activation of peroxisome proliferator-activated receptor (PPAR)delta promotes reversal of multiple metabolic abnormalities, reduces oxidative stress, and increases fatty acid oxidation in moderately obese men". Diabetes 57 (2): 332–9. doi:10.2337/db07-1318. PMID 18024853.
^ Normal 0 false false false EN-US X-NONE X-NONE GW-501516 GlaxoSmithKline/Ligand
^ "AICAR and GW 1516 - The Exercise Pill". Retrieved 2008-09-18.
^ Laurance J, Rajan A (2008-08-01). "Warning to Beijing Olympics over pills that mimic exercise". Health News, Health & Wellbeing. The Independent. Retrieved 2008-08-01.
^ WADA 2009 Prohibited List
