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G-4789 GW501516, Free Acid, >99%       Prices Reduced (June 2013)      NEW!

Synonyms:  [GSK-516] [GW1516] [GSK 516] [GSK516] [GW-1516] [GW 1516]

M.W. 453.50

C21H18F3NO3S2

[317318-70-0]

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO.  Disposal:  A

Find and View a Certificate of Analysis for this product

View the MSDS for this product

• GW501516 is a potent and selective peroxisome proliferator-activated receptor (PPAR) β/δ modulator.

• In vitro, GW501516 increased expression of the reverse cholesterol transporter ATP-binding cassette A1 and induced apolipoprotein A1-specific cholesterol efflux.  In vivo, GW501516 dramatically increased serum high density lipoprotein cholesterol while lowering the levels of small-dense low density lipoprotein, fasting triglycerides, and fasting insulin when dosed to insulin-resistant middle-aged obese rhesus monkeys.  Oliver, W.R. Jr., et al.  "A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport."  Proc. Natl. Acad. Sci. USA 98:  5306-5311 (2001).

• Treatment of skeletal muscle cells by GW501516 resulted in the expression of genes involved in lipid utilization, β-oxidation, cholesterol efflux, and energy uncoupling.  Furthermore, the treatment also increased apolipoprotein-A1 specific efflux of intracellular cholesterol, indicating the muscle tissue is an important target of PPARβ/δ agonists.  Dressel, U., et al.  "The peroxisome proliferator-activated receptor β/δ agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells."  Mol. Endocrinol. 17:  2477-2493 (2003).

• GW501516 induced fatty acid β-oxidation in L6 myotubes and in mouse skeletal muscles.  GW501516 treatment to mice fed a high-fat diet ameliorated diet-induced obesity as well as insulin resistance.  GW501516 treatment also dramatically improved diabetes, as demonstrated by the decrease in plasma glucose and blood insulin levels in genetically obese ob/ob mice.  Tanaka, T., et al.  "Activation of peroxisome proliferator-activated receptor δ induces fatty acid β-oxidation in skeletal muscle and attenuates metabolic syndrome."  Proc. Natl. Acad. Sci. USA 100:  15924-15929 (2003).

• GW501516 protected against cytotoxin-induced SH-SY5Y cell injury in vitro.  It also significantly attenuated the ischemic brain damage and MPTP-induced depletion of striatal dopamine and related metabolite contents in mouse brain.  Iwashita, A., et al.  "Neuroprotective efficacy of the peroxisome proliferator-activated receptor δ-selective agonists in vitro and in vivo."  J. Pharmacol. Exp. Ther. 320:  1087-1096 (2007).

• GW501516 treatment did not stimulate the growth of human cancer cell lines including HT29, HCT116, LS-174T, HepG2, and HuH7.  Hollingshead, H.E., et al.  "Peroxisome proliferator-activated receptor-β/δ (PPARβ/δ) ligands do not potentiate growth of human cancer cell lines."  Carcinogenesis 28:  2641-2649 (2007).

• GW501516 was identified as an orally active agent that would mimic or potentiate the effects of exercise.  Narkar, V.A., et al.  "AMPK and PPARδ agonists are exercise mimetics."  Cell 134:  405-415 (2008).

• GW 501516 reduced the IFNγ-induced up-regulation of TNFα and inducible NO synthase, and showed anti-inflammatory activity.  Defaux, A., et al.  "Effects of the PPAR-β agonist GW501516 in an in vitro model of brain inflammation and antibody-induced demyelination."  J. Neuroinflammation 6:  15 (2009).

• Another CAS number previously assigned to GW501516 free acid, namely 813458-54-7, has been deleted by CAS and is no longer in use.

• STRUCTURE ERROR ON WIKIPEDIA'S GW501516 PAGE:  As of December 21, 2012, the structure shown on the Wikipedia page for GW501516 is not correct -- the version shown on Wikipedia is missing a methyl group on the benzene ring carrying sulfur- and oxygen-bearing substituents.

• Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.

• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.

• Not available in some countries; not available to some institutions; not available for some uses.

** Our prices are lower than other vendors', but there is no compromise in quality.  Read how we are able to accomplish this:  Product Quality Discussion.

NOTES:
1.  The purpose of our competitor price comparison tables is to enable our visitors to compare the prices and purities of products of nominally equivalent quality, for vendors whose price and purity claims are openly available from a website or catalog (without a need for the customer to contact the vendor and request a quotation in order to obtain a price and purity for a standard product size).  However, the quality comparisons in these tables are not absolute:  although our product purities are uniformly very high and are established by careful testing of every lot in our laboratories, we cannot and do not vouch for the purities claimed by other vendors in these competitor price comparison tables.  (We do carry out occasional testing of other vendors' products -- see below --  and we have found many instances where vendors' product purities are far below their claimed levels.)  Effective April 1, 2011, our price comparison tables only include products where a purity commitment is found together with sizes and prices on at least one page of the vendor's web site.

2.  Researching and compiling sizes and prices for the >160 competitive vendors and more than 175 products is an expensive and tedious task for our small company.  Thus, we typically only perform revisions of these tables annually or less frequently.  The date and source of each competitive vendor's prices is indicated at the bottom of this page.  Obviously, we make no guarantee that competitive vendor prices will remain unchanged in the interval between our annual revisions.  We may occasionally update individual competitive vendor information and add new competitive vendors as we locate them.

3.  In some circumstances we permanently remove vendors from our price comparison tables.  Circumstances that lead to permanent removal are: 

A.  If a vendor does not honor its advertised price (ignoring small price increases) for one or more products when an order is attempted.  Example:  a vendor listed a compound at $808 for 10 grams on its website price list, but quoted $4,500 per 10 grams upon our inquiry.  That vendor has been permanently removed from our price comparison tables.

B.  If, on a product-by-product basis, our analyses of a vendor's product show purities more than a few percent below the vendor's advertised purities.  Example:  a vendor advertises a purity for 97% for a compound, but repeated elemental analyses show a minimum of 9% inorganic material present, beyond any salt counterion.  Another example: an HPLC analysis at a relevant UV detector wavelength shows 92% purity for a vendor's product for which 98% purity is claimed.  We realize of course that UV absorbances for impurities can be higher than for the main compound, but our products meet our purity commitment of typically >99% irrespective of absorbance factors for impurities, and we apply that standard to products from other vendors.

C.  Again on a product-by-product basis, if a vendor makes no purity claim for a given product, then their product is not shown on that product table.

D.  If we find that, as a pattern, several of a competitive vendor's products fail to meet their advertised purity commitments by significant margins or if a vendor does not provide standard and consistent purity claims for several of its products, then that vendor is permanently removed from all of our competitor price tables.

E.  Finally, if we determine that a vendor has provided fraudulent information on its website, in its literature or on a certificate of analysis, that vendor is permanently removed from all of our price comparison tables.

4.  IMPORTANT:  The presence of a competitive vendor entry in our price comparison tables does not necessarily mean that we have analyzed any of that vendor's products for purity; indeed, in most cases we have not.

5.  Please note:  where necessary, competitor prices are rounded to the nearest whole dollar.

To the best of our knowledge, the prices listed above for our competitors' products were correct as of the dates listed below for the sources of our annual price information update process.

Pricing Sources and Dates:  LC Labs - Current, Enzo Life Sciences - website - Jan 2013, AG Scientific - website - Jan 2013, Axxora - website - Jan 2013, Fluka - website - Dec 2012, Santa Cruz Biotech - website - Jan 2013, BioVision - website - Jan 2013, BePharm - website - May 2013, antibodies-online - website - Jan 2013, AOKBIO - website - May 2013, Ark Pharm - website - Dec 2012, Medchem Express - website - Jun 2013, ChemScene - website - Jan 2013.