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  1. #1
    Senior Member Times Roman's Avatar
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    GW 501516 "Exercise in a pill"

    Mates,
    I'll add to this later, and improve this information, but for now, here's a quick read to give you a basic understanding of this "peptide" (actually a PPAR), in that it improves endurance and helps reduce fat, amongst other things...

    http://en.wikipedia.org/wiki/GW501516

    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 10 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.

  2. #2
    Senior Member Times Roman's Avatar
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    GW501516 isn't as safe as some may think. A must read for those that want to know.

    http://www.unboundmedicine.com/medli...denoma_growth_

    Activation of nuclear hormone receptor peroxisome proliferator-activated receptor-delta accelerates intestinal adenoma growth.

    Abstract

    We treated Apc(min) mice, which are predisposed to intestinal polyposis, with a selective synthetic agonist of peroxisome proliferator-activated receptor-delta (PPAR-delta). Exposure of Apc(min) mice to the PPAR-delta ligand GW501516 resulted in a significant increase in the number and size of intestinal polyps. The most prominent effect was on polyp size; mice treated with the PPAR-delta activator had a fivefold increase in the number of polyps larger than 2 mm. Our results implicate PPAR-delta in the regulation of intestinal adenoma growth.


    Next:
    http://www.unboundmedicine.com/medli...rcinoma_cells_

    Title

    PPARdelta activation induces COX-2 gene expression and cell proliferation in human hepatocellular carcinoma cells.

    Abstract

    Cyclooxygenase-2 (COX-2) has been suggested to be associated with carcinogenesis. Recently, many studies have shown increased expression of COX-2 in a variety of human malignancies, including hepatocellular carcinoma (HCC). Therefore, it becomes important to know more about what determines COX-2 expression. In this work, we have studied the effect of PPARdelta activation on COX-2 expression using a selective agonist (GW501516) in human hepatocellular carcinoma (HepG2) cells. Activation of PPARdelta resulted in increased COX-2 mRNA and protein expression. The mechanism behind the induction seems to be increased activity of the proximal promoter of the COX-2 gene, spanning nucleotides -327 to +59. The increased COX-2 protein expression and promoter activity induced by the GW501516 was also confirmed in the monocytic cell line THP-1. Induced levels of COX-2 have previously been associated with resistance to apoptosis and increased cell proliferation in many cell types. In HepG2 cells, we observed a dose-dependent increase in cell number by GW501516 treatment for 72h. The levels of PCNA, used as an indicator of cell division were induced, and the cell survival promoting complex p65 (NF-kappaB) was phosphorylated under GW501516 treatment. We conclude that PPARdelta activation in HepG2 cells results in induced COX-2 expression and increased cellular proliferation. These results may suggest that PPARdelta plays an important role in the development of HCC by modulating expression of COX-2.

    Next...
    http://www.unboundmedicine.com/medli...rophage_cells_

    Title

    Evaluation of natural products on inhibition of inducible cyclooxygenase (COX-2) and nitric oxide synthase (iNOS) in cultured mouse macrophage cells.

    Abstract

    The inhibitors of prostaglandin biosynthesis and nitric oxide production have been considered as potential anti-inflammatory and cancer chemopreventive agents. In this study, we evaluated approximately 170 methanol extracts of natural products including Korean herbal medicines for the inhibition of prostaglandin E(2) production (for COX-2 inhibitors) and nitric oxide formation (for iNOS inhibitors) in lipopolysaccharide (LPS)-induced mouse macrophages RAW264.7 cells. As a result, several extracts such as Aristolochia debilis, Cinnamomum cassia, Cinnamomum loureirii, Curcuma zedoaria, Eugenia caryophyllata, Pterocarpus santalius, Rehmania glutinosa and Tribulus terrestris showed potent inhibition of COX-2 activity (>80% inhibition at the test concentration of 10 micro g/ml). In addition, the extracts of A. debilis, Caesalpinia sappan, Curcuma longa, C. zedoaria, Daphne genkwa and Morus alba were also considered as potential inhibitors of iNOS activity (>70% inhibition at the test concentration of 10 micro g/ml). These active extracts mediating COX-2 and iNOS inhibitory activities are warranted for further elucidation of active principles for development of new cancer chemopreventive and/or anti-inflammatory agents.


    To summarize, certain NSAIDS like Celebrex that are Cox2 inhibitors can minimize the risk. Unfortunately, Celebrex brings with it it's own risks. Additionally, if you go here, you can read about Cox2 inhibitors. You can make up your own mind which Cox2i is best for you. If you are real sharp, you will have noticed this passage:

    http://en.wikipedia.org/wiki/COX-2_inhibitor

    Also, Tribulus terrestris was shown to have strong inhibitory activity on COX-2.[5]

  3. #3
    Senior Member Four1Thr33's Avatar
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    Re: GW 501516 "Exercise in a pill"

    Have u or anyone used this product ... I have always had intrest from its first sell date but not read any user logs
    Wolves don't loose sleepover opinions of sheep

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    Re: GW 501516 "Exercise in a pill"

    Yep been on it for three months.

    Seem some weight loss but most important is my rise in endurance i get from it. Mind you I do it with 8-10oz of fresh organic beet juice

    I have bloods coming back, so it will also be interesting the effects on cholesterol.

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    Re: GW 501516 "Exercise in a pill"

    ive used it. works for endurance + fatloss. i have sarm search stuff.

  6. #6
    Senior Member Times Roman's Avatar
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    Re: GW 501516 "Exercise in a pill"

    Originally Posted by Four1Thr33 View Post
    Have u or anyone used this product ... I have always had intrest from its first sell date but not read any user logs
    I have not. I have 50 grams coming to me and should arrive here shortly......................

  7. #7
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    Re: GW 501516 "Exercise in a pill"

    after you use a vial take a break. after 4-5wks of use the positive effects fall off. so cycle it, in short runs

  8. #8
    Senior Member Times Roman's Avatar
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    Re: GW 501516 "Exercise in a pill"

    Originally Posted by gymrat827 View Post
    after you use a vial take a break. after 4-5wks of use the positive effects fall off. so cycle it, in short runs
    that's what i was hearing also. thanks for the heads up. make sure you read the warning label in #2 above.

  9. #9
    Elite Christosterone's Avatar
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    Re: GW 501516 "Exercise in a pill"

    I read somewhere that this was pulled from stage 2 trials, and the hcc potentiation may be why
    All posts are for entertainment purposes only

  10. #10
    Senior Member Times Roman's Avatar
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    Re: GW 501516 "Exercise in a pill"

    Originally Posted by Christosterone View Post
    I read somewhere that this was pulled from stage 2 trials, and the hcc potentiation may be why
    what we do in this lifestyle doesn't necessarily fall in lock step with the FDA. Not necessarily afraid of it being pulled from a trial. Being fully informed is my prime concern.

    You don't have a link, do you?

  11. #11
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    Re: GW 501516 "Exercise in a pill"

    Stay away from that shit guys, can really mess with your heart. If you really want all the same benefits with no sides, start injecting high concentrated l-carnitine.

  12. #12
    Senior Member Times Roman's Avatar
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    Re: GW 501516 "Exercise in a pill"

    Originally Posted by Supra View Post
    Stay away from that shit guys, can really mess with your heart. If you really want all the same benefits with no sides, start injecting high concentrated l-carnitine.
    Not to be antagonistic or disresectful, but do you have a link to support that claim?

    Here is a link to suggest otherwise... (there are others)

    http://circ.ahajournals.org/content/118/10/1021.full

  13. #13
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    Re: GW 501516 "Exercise in a pill"

    Did you just post about this at steroids.com?
    "Luvbytes tipped me off to this information. Kudos go to him.....

    http://www.unboundmedicine.com/medli...denoma_growth_


    Activation of nuclear hormone receptor peroxisome proliferator-activated receptor-delta accelerates intestinal adenoma growth.

    Abstract

    We treated Apc(min) mice, which are predisposed to intestinal polyposis, with a selective synthetic agonist of peroxisome proliferator-activated receptor-delta (PPAR-delta). Exposure of Apc(min) mice to the PPAR-delta ligand GW501516 resulted in a significant increase in the number and size of intestinal polyps. The most prominent effect was on polyp size; mice treated with the PPAR-delta activator had a fivefold increase in the number of polyps larger than 2 mm. Our results implicate PPAR-delta in the regulation of intestinal adenoma growth.


    Next:

    http://www.unboundmedicine.com/medli...rcinoma_cells_


    Title

    PPARdelta activation induces COX-2 gene expression and cell proliferation in human hepatocellular carcinoma cells.

    Abstract

    Cyclooxygenase-2 (COX-2) has been suggested to be associated with carcinogenesis. Recently, many studies have shown increased expression of COX-2 in a variety of human malignancies, including hepatocellular carcinoma (HCC). Therefore, it becomes important to know more about what determines COX-2 expression. In this work, we have studied the effect of PPARdelta activation on COX-2 expression using a selective agonist (GW501516) in human hepatocellular carcinoma (HepG2) cells. Activation of PPARdelta resulted in increased COX-2 mRNA and protein expression. The mechanism behind the induction seems to be increased activity of the proximal promoter of the COX-2 gene, spanning nucleotides -327 to +59. The increased COX-2 protein expression and promoter activity induced by the GW501516 was also confirmed in the monocytic cell line THP-1. Induced levels of COX-2 have previously been associated with resistance to apoptosis and increased cell proliferation in many cell types. In HepG2 cells, we observed a dose-dependent increase in cell number by GW501516 treatment for 72h. The levels of PCNA, used as an indicator of cell division were induced, and the cell survival promoting complex p65 (NF-kappaB) was phosphorylated under GW501516 treatment. We conclude that PPARdelta activation in HepG2 cells results in induced COX-2 expression and increased cellular proliferation. These results may suggest that PPARdelta plays an important role in the development of HCC by modulating expression of COX-2.

    Next...

    http://www.unboundmedicine.com/medli...rophage_cells_


    Title

    Evaluation of natural products on inhibition of inducible cyclooxygenase (COX-2) and nitric oxide synthase (iNOS) in cultured mouse macrophage cells.

    Abstract

    The inhibitors of prostaglandin biosynthesis and nitric oxide production have been considered as potential anti-inflammatory and cancer chemopreventive agents. In this study, we evaluated approximately 170 methanol extracts of natural products including Korean herbal medicines for the inhibition of prostaglandin E(2) production (for COX-2 inhibitors) and nitric oxide formation (for iNOS inhibitors) in lipopolysaccharide (LPS)-induced mouse macrophages RAW264.7 cells. As a result, several extracts such as Aristolochia debilis, Cinnamomum cassia, Cinnamomum loureirii, Curcuma zedoaria, Eugenia caryophyllata, Pterocarpus santalius, Rehmania glutinosa and Tribulus terrestris showed potent inhibition of COX-2 activity (>80% inhibition at the test concentration of 10 micro g/ml). In addition, the extracts of A. debilis, Caesalpinia sappan, Curcuma longa, C. zedoaria, Daphne genkwa and Morus alba were also considered as potential inhibitors of iNOS activity (>70% inhibition at the test concentration of 10 micro g/ml). These active extracts mediating COX-2 and iNOS inhibitory activities are warranted for further elucidation of active principles for development of new cancer chemopreventive and/or anti-inflammatory agents."

  14. #14
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    Re: GW 501516 "Exercise in a pill"

    Originally Posted by Times Roman View Post
    Not to be antagonistic or disresectful, but do you have a link to support that claim?

    Here is a link to suggest otherwise... (there are others)

    http://circ.ahajournals.org/content/118/10/1021.full
    Those links support angiogenesis, which is a good and bad thing, bad for you if you have a tumor, but it has been shown to induce growth in the heart..which isn't a good thing
    All posts are for entertainment purposes only

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    Re: GW 501516 "Exercise in a pill"

    Originally Posted by Christosterone View Post
    Those links support angiogenesis, which is a good and bad thing, bad for you if you have a tumor, but it has been shown to induce growth in the heart..which isn't a good thing
    Exactly, people take shit then come to these forums and make a big stink about shady grey market products..then when we don't agree they want to argue about it..this stuff is dangerous and will be a no thought iin 3 month's time when the next shady chem comes out.

  16. #16
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    Re: GW 501516 "Exercise in a pill"

    I read that it might of been dropped in stage 2 of trials, I'm trying to find the link, but as times did post it can promote HCC (type of liver cancer or hepatocellular carcinoma) also, the angiogenesis can be a good thing or a bad thing. If people didn't die of heart attacks or infxns, we would all eventually die of cancer, our DNA takes too much abuse through the years, which is why in older years, angiogenesis is bad (some rumors actually secrete growth factors that promote angiogenesis so they can spread) and enlarged heart is no good either. IMO, it's a young mans peptide, unless you've been through a pet scan clearing any tumor growth.

    Preach
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    Re: GW 501516 "Exercise in a pill"

    This is all a good read, what precautions should one take while running GW?

  18. #18
    Senior Member Times Roman's Avatar
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    Re: GW 501516 "Exercise in a pill"

    Originally Posted by TheMinister View Post
    This is all a good read, what precautions should one take while running GW?
    when my GW powder comes in, i'll be capping and mixing with tribulus. I'll have to look it up again, but i'm thinking a gram of tribulus a day will minimize the risk of stomach polyps. Additionally, this is not something you take forever. A month on, a month off, that sort of thing.

    As others have correctly pointed out, this is still some pretty new stuff, and maintaining an air of caution is prudent.

    If you don't want to run the tribulus, a cox2i such as celebrex works too, although celebrex brings some mild risks as well.

  19. #19
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    Re: GW 501516 "Exercise in a pill"

    Ya, it seems like its best for cutting phase, but due to its sta ding in becoming a scripted drug being pulled (I believe) there has to be some caution, thanks for info roman
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  20. #20
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    Re: GW 501516 "Exercise in a pill"

    Thanks roman, I've been on 3 mths time to take a break for a month!

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