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What is Gw-1516?
GW501516 is a selective agonist (activator) of the PPARδ receptor.[19] It displays high affinity (Ki = 1 nM) and potency (EC50 = 1 nM) for PPARδ with > 1000 fold selectivity over PPARα and PPARγ.[13]
In rats, binding of GW501516 to PPARδ recruits the coactivator PGC-1α. The PPARδ/coactivator complex in turn upregulates the expression of proteins involved in energy expenditure.[20] Furthermore in rats treated with GW501516, increased fatty acid metabolism in skeletal muscle and protection against diet-induced obesity and type II diabetes was observed. In obese rhesus monkeys, GW501516 increased high-density lipoprotein (HDL) and lowered very-low-density lipoprotein (VLDL).[20] The mechanism by which PPARδ agonists increase HDL appears to be a result of increased expression of the cholesterol transporter ABCA1.[5]
Gw-1516 Dosage
Typical Gw-1516 Dosage is anywhere from 10-100mgs a day, with the average being between 10-20mgs a day. The half life is 24 hours.
5.
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Click here to buy Gw-1516 / Gw-501516 Raw powder - from Hardcore Powders!
What is Gw-1516?
GW501516 is a selective agonist (activator) of the PPARδ receptor.[19] It displays high affinity (Ki = 1 nM) and potency (EC50 = 1 nM) for PPARδ with > 1000 fold selectivity over PPARα and PPARγ.[13]
In rats, binding of GW501516 to PPARδ recruits the coactivator PGC-1α. The PPARδ/coactivator complex in turn upregulates the expression of proteins involved in energy expenditure.[20] Furthermore in rats treated with GW501516, increased fatty acid metabolism in skeletal muscle and protection against diet-induced obesity and type II diabetes was observed. In obese rhesus monkeys, GW501516 increased high-density lipoprotein (HDL) and lowered very-low-density lipoprotein (VLDL).[20] The mechanism by which PPARδ agonists increase HDL appears to be a result of increased expression of the cholesterol transporter ABCA1.[5]
Gw-1516 Dosage
Typical Gw-1516 Dosage is anywhere from 10-100mgs a day, with the average being between 10-20mgs a day. The half life is 24 hours.
5.
- ^ Jump up to:[SUP]a[/SUP] [SUP]b[/SUP] 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.
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- ^ Jump up to:[SUP]a[/SUP] [SUP]b[/SUP] Oliver WR, Shenk JL, Snaith MR, Russell CS, Plunket KD, Bodkin NL, Lewis MC, Winegar DA, Sznaidman ML, Lambert MH, Xu HE, Sternbach DD, Kliewer SA, Hansen BC, Willson TM (April 2001). "A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport". Proc. Natl. Acad. Sci. U.S.A. 98 (9): 5306–11.doi:10.1073/pnas.091021198. PMC 33205. PMID 11309497.
- Jump up to:[SUP]a[/SUP] [SUP]b[/SUP]Oliver WR, Shenk JL, Snaith MR, Russell CS, Plunket KD, Bodkin NL, Lewis MC, Winegar DA, Sznaidman ML, Lambert MH, Xu HE, Sternbach DD, Kliewer SA, Hansen BC, Willson TM (April 2001). "A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport". Proc. Natl. Acad. Sci. U.S.A. 98 (9): 5306–11.doi:10.1073/pnas.091021198. PMC 33205. PMID 11309497.
- ^ Jump up to:[SUP]a[/SUP] [SUP]b[/SUP] Sprecher DL (December 2007). "Lipids, lipoproteins, and peroxisome proliferator activated receptor-delta". Am. J. Cardiol. 100 (11 A): n20–4. doi:10.1016/j.amjcard.2007.08.009.PMID 18047848.
