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GW-501516 (also known as GW-501,516, GW1516 or GSK-516) is a PPARδ modulator compound being investigated for drug use by GlaxoSmithKline.[1][2] It activates the same pathways activated through exercise, including PPARδ 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 for GW-501516 and other related PPARδ 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.
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ShaneV wrote: Sounds promising. You be the guinea pig, and keep the rest of us informed.
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spartacus wrote: does sound awesome admin, what form does it come in?
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admin wrote:
ShaneV wrote: Sounds promising. You be the guinea pig, and keep the rest of us informed.
Welcome to the forum, but to be honest I'll rather see someone else use it before me. But on the other hand it seems to be beneficial to HDL cholesterol increases.
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AICAR en GW1516 is dieselfde ding. Eintlik is dit GW501516. Dit is 'n Peroxisoom-Proliferator-geaktiveerde Reseptor-delta analoog of kortweg 'n PPAR-delta. Dis 'n molekule wat tot 'n mate "uncoupling" doen deurdat dit vetsure uit adipose weefsel verbrand eerder as koolhidrate as bron van energie vanuit speir weefsel. Dit beskerm eintlik die pankreas teen oormatige insulien sekresie tydens oefening deur onder andere insulien sensitiwiteit op spierselle te verbeter. Dus mobiliseer dit die vry vetsure makliker en maak dan ook die beskikbare insulien molekules meer sensitief om eerder vetsure oor die spiersel membrane te vervoer as glukose.
En dit is waar die performance enhancement inkom. Vet verbranding lewer baie meer energie vir baie langer as wat koolhidraat verbranding doen. Endurance atlete se metabolismes is geneties aangepas om vet te verbrand by voorkeur bo koolhidrate. Die in vitro studies het gewys aanvanklik 'n verbetering van 44% in die vet verbranding kapasiteit.
Rondom toetsing vir die AICAR molekule? Anti-Doping weet reeds daarvan. Die Duitsers het die bestaan van die molekule alreeds in 2009 beskryf en reeds toe al die endurance enhancement uitgewys. Of hulle al 'n toets het ddaarvoor weet ek nie, want die flippin artikel is in Duits geskryf en ek kan Duits lees, maar kon nie die volle abstract afgetrek kry nie.
Maar, ouboet, hier's eerder iets meer interessants. Gaan doen 'n search vir Follistatin - dis 'n myostatin-antagonist waaraan die ouens tans werk. Dit word lokaal ingespuit, veroorsaak gene-expression vir spier hipertrofie, maar slegs vir skelet spier. En, hier's die nice deel... Anders as met AAS, veroorsaak Follistatin PERMANENTE spier hipertrofie. Hmmn, heel interessant...
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Roozer wrote: good day guys
tell me admin the follistatin the grocer said it comes in a 20iu vail which is 18mg is this correct ?
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admin wrote: I he also taking AICAR with the GW501516?
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MK wrote: Looking forward to reading your Myostatin HMP 250 cycle log, Yohimbe!
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