GW1516, also known as GW501516

GW 501516
From Wikipedia, the free encyclopedia

GW-501,516 (also known as GW1516 or GSK-516) is a drug developed by GlaxoSmithKline, which acts as a PPARδ modulator.[1][2] It activates AMP-activated protein kinase and stimulates glucose uptake in skeletal muscle tissue,[3] and has been demonstrated to reverse metabolic abnormalities in obese men with pre-diabetic metabolic syndrome, most likely by stimulating fatty acid oxidation.[4] It has been proposed as a potential treatment for obesity and related conditions,[5] especially when used in conjunction with a synergistic compound AICAR, as the combination has been shown to significantly increase exercise endurance in animal studies.[6][7]
Concerns were raised prior to the 2008 Beijing Olympics that GW-501,516 or the GW-501,516 / AICAR combination 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.[8] The World Anti-Doping Agency has also begun work on a test for the two drugs,[9] and they have been added to the prohibited list from 2009 onwards.[10]

1 ^ 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.
2 ^ 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.
3 ^ 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.
4 ^ 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.
5 ^ 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. PMID 16511591.
6 ^ 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 PPARδ Agonists Are Exercise Mimetics" (PDF). Cell 134: 1–11. doi:10.1016/j.cell.2008.06.051.
7 ^ "Exercise In A Pill: Researchers Identify Drugs That Enhance Exercise Endurance". Science News. ScienceDaily. 2008-08-01. Retrieved 2008-08-01.
8 ^ "AICAR and GW 1516 - The Exercise Pill". Retrieved 2008-09-18.
9 ^ 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.
10 ^ WADA 2009 Prohibited List
 
The AMP-activated protein kinase (AMPK) cascade is a
sensor of cellular energy status. Whenever the cellular
ATP:ADP ratio falls, owing to a stress that inhibits ATP
production or increases ATP consumption, this is amplified
by adenylate kinase into a much larger increase in the
AMP:ATP ratio. AMP activates the system by binding to
two tandem domains on the​
g subunits of AMPK, and this
is antagonized by high concentrations of ATP. AMP
binding causes activation by a sensitive mechanism
involving phosphorylation of AMPK by the tumour
suppressor LKB1. Once activated, AMPK switches on
catabolic pathways that generate ATP while switching off
ATP-consuming processes. As well as acting at the level of
the individual cell, the system also regulates food intake
and energy expenditure at the whole body level, in
particular by mediating the effects of hormones and
cytokines such as leptin, adiponectin and ghrelin. A
particularly interesting downstream target recently
identified is TSC2 (tuberin). The LKB1
®AMPK®TSC2
pathway negatively regulates the target of rapamycin
(TOR), and this appears to be responsible for limiting
protein synthesis and cell growth, and protecting against
apoptosis, during cellular stresses such as glucose

starvation.
 
OK guys here we are
this is my take on Aicar & GW1516 here is my take on this shit,,, and i mean piece of shit i spent a lot of money for 3 of my friends guinea pig and my on guinea pig... all of them allready had a great performance... no possitive signs of making any better performance then already had... i mean nothing after 3 months.... but but look out for the damages done to your body....
look ou for the HDL to go seriously low careful or you'll have some serious problems... heart palpitation and serious Arrhythmia Possible symptoms of a common type of arrhythmia, a trial fibrillation, include heart palpitations, dizziness, and chest pain pinching and other... </SPAN>
it decreased VO max in all 4 of them
it seams to run out stamina faster than normal, recovery prolonged the time, it seams that lungs and heart was affected by it…
so overall performance has not been enhanced
on the other hand it has damaged performance in all 4 guinea pig
protocol followed was 1 month 2 time a week 100mg
no improvement but loss of performance was seen then
change protocol to 3 times a week same thing happen.
Then third month change protocol to 8 days 13 mg a day 2 days of for 40 days.
Same shit loss of performance…..
Some is not right with this crappie product some has to be changed… some is not right for sure
My advice stay a way from it for the moment until they get it right…
<!-- / message -->
 
It is a very harmful useless peptide with NO KNOWN PROOF !! I would advise NO ONE USE THIS Until further evidence proves otherwise.. That's ENGLISH for you.
 
Starting my rat on GW 501516 tomorrow. this thread had caused me concern for his health but reading a study published in the diabetes journals.org has swayed me to begin research. A snippet below I found very interesting. Basically states there were no side effects from GW501516 besides one participant developing a rash after administration. Dosage appears to be capped at 10mgs. Good cholesterol remained unchanged, bad and total cholesterol was lowered as was triglyceride levels. participant weight and liver fat were also decreased while insulin sensitivity increased as was fat oxidation.

Full article:
Activation of Peroxisome Proliferator?Activated Receptor (PPAR)? Promotes Reversal of Multiple Metabolic Abnormalities, Reduces Oxidative Stress, and Increases Fatty Acid Oxidation in Moderately Obese Men
RESULTS

There were no significant differences between the three groups after randomization. Thus, age, blood pressure, total cholesterol, apoB, HDL cholesterol, and triglycerides were balanced between groups (Table 1). There was no difference in baseline ALT and AST concentrations between the groups (Table 1). Three of six subjects in the GW501516- and GW590735-treated groups fulfilled the The National Cholesterol Education Program Adult Treatment Panel III criteria for the metabolic syndrome (39), whereas two of six fulfilled the criteria in the placebo group.
Tolerability.

There were no significant symptomatic side effects, and the results of liver (AST and ALT), hematology (blood cell counts), and renal function (creatinine) tests were unchanged in all groups. The concentration of γGT was unchanged in the placebo and GW590735 groups, but a 23% (P < 0.05) lowering was seen in response to GW501516 treatment (Table 2).
One subject developed a skin rash within 24 h after the first dose of GW590735, leading to withdrawal from the study. Treatment allocation for this patient remained concealed after this event, and a new subject was recruited to continue the study with the same blinded treatment allocation. Body weights did not change in placebo and GW590735-treated subjects, whereas subjects treated with GW501516 tended to lose weight (−1.7 ± 0.7 kg, P = 0.05) over the 2-week treatment period.
Fasting plasma metabolic characteristics.

Total and LDL cholesterol were reduced by 20 and 23%, respectively (both P < 0.05), accompanied by a 21% lowering of apoB (P < 0.05) in subjects receiving GW501516 (Table 2). HDL cholesterol was unchanged. Triglycerides were lowered by 31% (P < 0.05). There was a very distinct lowering of fasting plasma NEFA (−40%, P < 0.01). The lowering of NEFA was supported by significant lowering (−25%, P < 0.05) of fasting plasma glycerol (data not shown). Treatment with GW590735 resulted in a similar reduction in fasting plasma triglycerides (−27%, P < 0.05) but no change in NEFA (Table 2) or glycerol (data not shown). LDL cholesterol did not change significantly, whereas a modest reduction in apoB (−13%, P < 0.05) was observed with GW590735. HDL cholesterol tended to increase. Corresponding changes in lipids and lipoproteins in placebo-treated subjects were small and not statistically significant.
Fasting plasma insulin concentration was slightly reduced in response to GW501516 together with a small reduction in fasting plasma glucose (P < 0.05). This led to a significantly improved insulin sensitivity, calculated as homeostasis model assessment of insulin resistance (40), which was not seen in the GW590735 and placebo groups (Table 2).
Liver fat.

There was no statistically significant difference in liver fat content between the groups at baseline. The GW501516-treated group exhibited a 20% reduction in liver fat that was statistically significant after adjustment for baseline fat content (Fig. 1). Liver fat content in both GW590735-treated and placebo subjects tended to increase during the treatment period; neither of these changes were statistically significant.
 
Rats 1st Day - hit same lifts Ive been doing past 3 weeks. Been feeling a plateau; perhaps even fatigued. Anyway - 10mgs of GW501516 and 25mgs of MK2866 an hour before their usual evening workout. They said both taste like complete ass but half a ml of each was ok to get down. Felt no different prior to the gym. First stop was machine bench. Felt strong, but not enough to say it was noticeable, until the 4th set. was feeling ready to hit it again earlier than normal. perhaps attributable to placebo effect. I will say I started to get a wicked good pump in the chest; noticeably better than the usual.

Next was machine fly. Starting at last Thursday's weight it felt way too easy; and after I had just hammered slightly heavier machine bench. I moved weight up 15%. Still felt easier than normal but I stuck w/ it to see what I could do. This is where things got weird. My reps were INCREASING w/ same weight. I know I wasnt 'pushing myself harder' as I was reping to failure on it and was doing the same yesterday. With lower weight on Thursday reps started at 12 and over 5 sets dropped to 8 maintaining same weight. Here I was able to move weight up 15%, 14 reps, 12 reps, 13 reps, 14 reps, 15 reps. Never lifted to failure before and had reps increasing. That was what sold me that one of these compounds was having an impact and seemed to be really kicking in 1.5 hours after administration. Only food prior was mid calorie protein/creatine shake .5 hours prior to workout.
<O:p></O:p>
Workout continued in hitting tri's w/ dumbbell pullovers and machine tri extension. hadnt done dumbbell pullover in a while but it felt good but unfortunately I couldnt compare vs prior weeks reps/weight. Machine tri extension I was up on weight but could have been due to switching the lift prior to it. Anyway - again a crazy pump in tri's. Havent had a pump like that since I was on cycle; and the pump then might not have even been quite what it was last night.
<O:p></O:p>
Immediately after lifts hit treadmill. Typically have about a mile in the gas tank after lifting, and wasnt expecting much more especially w/ all the blood up in the chest and tri's. Typical run looks like run .5 mile @7mph, walk .2mile @ 2.5mph, run .3mile @10-11 mph. Can usually get BPM to hit 160-170 on the first section and 180 on the 'sprint' (my rats HATE running). Felt good after first .5 miles, extended the 7mph section to .8miles, felt 'good' faster and got my bpm back down under 130 after only .10miles of walking so rested there until .15miles. Sprint extended to .4miles as I was breathing slower and more controlled than usual at 11mph. Still hit 180bpm after sprint but took materially less time to get back down under 130bpm.
<O:p></O:p>
I am skeptical by nature, and could probably assign much of this to placebo effect if not for the fact that I have been in the same 'rut' for 2 weeks where weights had been static and running just sucking. Ive never moved through sets increasing reps when lifting to failure and weight constant; I still cant get over that. Running was still not fun but there was more in the tank and definitely faster recovery time to get heart rate down. I cannot assign the measurement of my heart rate reduction to placebo I dont think. And for the fact, I left the gym I felt like I wanted to turn around and do it all again.... this was great.
<O:p></O:p>
Its only been ONE DAY though, and one point does not a line make. Will be hitting it more through the week so will surely report back on this. Maybe I need to start this as its own thread/log. Also, unfortunately my rats dont have the patience to test only one of the compounds individually to isolate effects so youll have to keep that in mind. Not sure if weight increases were assignable to MK2866 and running to GW50 or MK2866 was all of it and GW50 is useless or vice versa; this 'log' is for the stack of the two. No sides to report except the shitty taste of both (they tasted identical to me) and oddly when completing bench I noticed my nips were glass cutters which I dont recall happening recently either...
 
Last edited:
Second day on; definitely more punch at the gym. Unfortunately I ate prior to working out due to an impromtu celebration by my office. That typically kills my workouts having sliders and wings before hitting weights and cardio. While I wasnt quite as amped as the prior day my tank felt full. all weights were up for back and bi's from Friday of last week; where I had been fairly constant the prior 2 weeks. I even pulled something that I never would do;/ I split back and delts and went up and did cardio as there was an exotic little lady on the treadmill working out in booty shorts and stockings. Im sure that was motivation to jump on the bike behind her for 30 mins. After I got bored and beat I went back down to finish up bi's. Remarkably I still felt strong. Usually and cardio before a lift kills me. After bi's I went back upstairs to hit the treadmill and matched yesterday's performance w/o any fall off. Left the gym feeling still energized. lovin' this stuff.

still no sides. nips hard, noticed I was feeling more hot than usual; feeling pretty warm again this morning still. might actually be a slightly decreased appetite as well. typically have a big breakfast, then I work out for my lunch instead of eating and instead grab half a tub of cottage cheese before the day is out or I feel faint. I didnt get hungry once yesterday. had to force down some food at the office function. maybe not a good side if you are trying to gain on this stuff. Probably best used in a cutting or bridging program.
 
what are sliders bro?
haha - sliders Presser. they are mini burgers. not typical food for me when Im trying to clean up but Id have looked like an ass in front of our partners being the only guy not eating. I hate eating close to lifting; kills my workouts. the mini burgers were held to minimal damage. I was somehow able to avoid the open bar.
 
haha - sliders Presser. they are mini burgers. not typical food for me when Im trying to clean up but Id have looked like an ass in front of our partners being the only guy not eating. I hate eating close to lifting; kills my workouts. the mini burgers were held to minimal damage. I was somehow able to avoid the open bar.

lol, good man! Im not a big fan of alcohol, but i will throw down some vodka! lol
 
haha - sliders Presser. they are mini burgers. not typical food for me when Im trying to clean up but Id have looked like an ass in front of our partners being the only guy not eating. I hate eating close to lifting; kills my workouts. the mini burgers were held to minimal damage. I was somehow able to avoid the open bar.

So far you would recommend it?
 
Yes! most definitely! Sorry I have been off this board for a while; the switch to the new site lost my auto-login and I couldnt figure out where the hell the 'forgot password' link was. finally got it!

Anyway - yes. As I discussed in my initial post when I started I had hit a plateau. Since I beginning the MK2866 and the GW501516 my weights and reps have continued to increase and I have put on a quarter inch on my arms now at about 17 3/4". The initial punch I got to my workouts I cant say with certainty wasnt sort of a placebo effect or not since that has somewhat abated. However, I have been getting great pumps still, and like I said, the progress in weight/reps cant be denied. I havent changed anything from what I was doing before; not even diet. been growing and becoming slightly more defined. if my diet wasnt so 'dirty' I bet Id make a lot more progress here. One thing; I was seeing huge progress in my cardio for the first week or two - that has seemed to stop but I am still doing much further/much faster runs on the treadmill. havent changed dosage still 10mgs GW501516 and 25mgs MK2866. no sides to report; sex drive still good, appetite intact, sleeping fine, skin on face might be a little more oily than usual but not much. I did take my blood pressure at the drug store several times since my last blood work and it has dropped noticeably from 130's/80's to 115-ish/70-ish. GW501516 is supposed to help good cholesterol and BP so that is a great side for me :)

all in all this would seem to me to be a great 'bridge' for someone trying to maintain, or even build a little between cycles. some people have said MK2866 it is mildly supressive to test at higher doses so I probably wouldnt run it w/ PCT if I was trying to get my natty up quick.

I would be curious what difference there would be if I ran one independant of the other but I dont want to risk wasting my time testing my rat w/ half effectiveness just for the sake of identifying which effects are from which compound. they arent really that much to get together and I like the results Im seeing from it.
 
let us know your results. i'll save my opinion til then. i know some guys who have used this also

So MR - what was your opinion on this specifically (GW501516) or also MK2866 'Ostarine' if you have any input on that as well? Curious what you have seen/heard or experienced.
 
Back
Top