# GW 501516 "Exercise in a pill"



## Times Roman

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.


----------



## Times Roman

*GW501516 isn't as safe as some may think. A must read for those that want to know.*

http://www.unboundmedicine.com/medl..._delta_accelerates_intestinal_adenoma_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/medl...tion_in_human_hepatocellular_carcinoma_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/medl...se__iNOS__in_cultured_mouse_macrophage_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]


----------



## Four1Thr33

Have u or anyone used this product ... I have always had intrest from its first sell date but not read any user logs


----------



## theminister

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.


----------



## gymrat827

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


----------



## Times Roman

Four1Thr33 said:


> 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......................


----------



## gymrat827

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


----------



## Times Roman

gymrat827 said:


> 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.


----------



## Christosterone

I read somewhere that this was pulled from stage 2 trials, and the hcc potentiation may be why


----------



## Times Roman

Christosterone said:


> 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?


----------



## Supra

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.


----------



## Times Roman

Supra said:


> 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


----------



## Supra

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."


----------



## Christosterone

Times Roman said:


> 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


----------



## Supra

Christosterone said:


> 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.


----------



## Christosterone

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


----------



## theminister

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


----------



## Times Roman

TheMinister said:


> 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.


----------



## Christosterone

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


----------



## theminister

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


----------



## Times Roman

TheMinister said:


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



Probably a good idea


----------



## Tim

Supra. What amount would you suggest with the I-carn?


----------



## grizzldsealpoacher

I used it 90 day run 5mg per I started 267lbs 35%bf + first 8 weeks had a 5 to 7 lb drop per wk  with proper diet Cardio increased became alot ezier doubled in 8 wks no strength increase maybe a little endurance. I had a lipid panel done b4 and it was horrible do to some abuse of winni as a newb or really a non exist b/c I didnt know about forums yet 273 over all 12 hdl 

results after 8 wks 227lbs down to about 17% bf lipids were 103 overall 27hdl  after this point weight loss slowed lipids i didnt have re tested seemed like my body got used to


----------



## Four1Thr33

40lb drop in 8 weeks is a ton.  Congrats bro.


----------



## Times Roman

grizzldsealpoacher said:


> I used it 90 day run 5mg per I started 267lbs 35%bf + first 8 weeks had a 5 to 7 lb drop per wk  with proper diet Cardio increased became alot ezier doubled in 8 wks no strength increase maybe a little endurance. I had a lipid panel done b4 and it was horrible do to some abuse of winni as a newb or really a non exist b/c I didnt know about forums yet 273 over all 12 hdl
> 
> results after 8 wks 227lbs down to about 17% bf lipids were 103 overall 27hdl  after this point weight loss slowed lipids i didnt have re tested seemed like my body got used to it
> 
> 
> heres the log



when i'm fat and not lifting, i can lose about 30lbs in two months on the atkins, or about a half pound a day.  no cardio, no starving, just eat til satiated.  atkins is NOT good when resistance training.

but, when you said your body seemed to get used to it, it probably did.  another reason for alternating months when taking it.....?


----------



## Four1Thr33

Ya I lost 50 in 4 months on Atkins.   It's amazing diet I might need to try again


----------



## Times Roman

Four1Thr33 said:


> Ya I lost 50 in 4 months on Atkins.   It's amazing diet I might need to try again



when  i"m NOT lifting, i['ll go 2 months on atkins, then switch to a south beach,  at which point, i CAN lift.


----------



## Four1Thr33

I am taking time off for injury recovery starting a few days ago... Atkins might be in my future again before next cycle... I just need to rebuild a diet I don't think I had enough cals last time


----------



## Times Roman

Four1Thr33 said:


> I am taking *time off for injury recovery *starting a few days ago... Atkins might be in my future again before next cycle... I just need to rebuild a diet I don't think I had enough cals last time



looking into TB?


----------



## Four1Thr33

I was shopping yes but I have not pulled the trigger yet due to close to a grand this month in Raws and gear.   But 4 days off and yup still hurts


----------



## Tim

I have been on this for three weeks. The sides, which at first I thought was stomach flu and Bronchitis, included nausea sore throat reflux and some pulmonary resistance.  I wonder if it is a factor of the suspension or dose?  I was using 10mg ed. Any feedback appreciated


----------



## Tim

BTW my endurance is phenomenal and recover amazing. I would be interested in a powder source or anything that is not like the Satan's piss that is the suspension used in my suppliers brew


----------



## Times Roman

I'm using a another source, and have secured two bottles of GW.  I'll be starting on the first and will be keeping a log.  My goal would be to drop BF%.  I'll be more specific in the log.


----------



## Times Roman

I thought I was keeping a log here.  I've used two bottles of GW over a 40 day period.

unfortunately, I wasn't impressed.

Expensive

Little or no result.

I think it zapped alot of my strength

Very moderate cardio improvement

Really didn't lose much BF, evenwith the extended cardio

I won't be trying it again.

Looking into T3/albuterol next


----------



## gymrat827

you should of stopped at the first bottle, gave it a 20 day break and then use the 2nd.  


i had good results from T3/Alb fyi......


----------



## Times Roman

gymrat827 said:


> you should of stopped at the first bottle, gave it a 20 day break and then use the 2nd.
> 
> 
> i had good results from T3/Alb fyi......



I may have been dosing higher than 1ml/day (5mg/ml) since I ran out a week earlier than i thought, either that, or the bottle didn't have the full 30ml.  so i doubled the dose and ran out the second bottle in a little under two weeks.  total time was about 5 weeks.  i understand the 30 days on and 30 off, but 5 weeks is close enough for me.

btw, now that I'm off the GW, strength is returning


----------



## Tubby2

*source for 516?*

Do you have a trustworthy source for 516? Could you share that? or PM me with it?



theminister said:


> 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.


----------



## AlexTim

GW is good for burning fat. The study is quoted stating: “physiological and pathophysiological functions of PPAR and generated novel strategies to treat metabolic diseases”.The activation of these particular genes in the body has been seen to burn body fat at such an alarming rate that it is being coined “the cure for obesity”.
There were absolutely no adverse side effects detected in the last 20 years of study and it was extremely rare to see muscle wasting at any point during the research.


----------



## Jin

AlexTim said:


> GW is good for burning fat. The study is quoted stating: “physiological and pathophysiological functions of PPAR and generated novel strategies to treat metabolic diseases”.The activation of these particular genes in the body has been seen to burn body fat at such an alarming rate that it is being coined “the cure for obesity”.
> There were absolutely no adverse side effects detected in the last 20 years of study and it was extremely rare to see muscle wasting at any point during the research.



I can't find any GW........where do I get it?


----------



## Bro Bundy

Times roman pm


----------

