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Postion:Product Catalog >API>Inhibitors>GW-501516
GW-501516
  • GW-501516
  • GW-501516
  • GW-501516
  • GW-501516
  • GW-501516

GW-501516 NEW

Price Get Latest Price
Package 1KG 5KG 25KG
Min. Order: 1KG
Supply Ability: 20 T each week
Update Time: 2023-08-23

Product Details

Product Name: GW-501516 CAS No.: 317318-70-0
EC-No.: 1592732-453-0 Min. Order: 1KG
Purity: 98%~99% Supply Ability: 20 T each week
Release date: 2023/08/23

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Product Name:GW-501516
Synonyms:2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid;GW 501516, >=98%;ENDUROBOL (GW-501516)/CARDARINE/;Cardarine(GW501516, GSK-516);GW-501615;CB6465728;2-(4-((2-(4-(Trifluoromethyl)phenyl)-4-methylthiazol-5-yl)methylthio)-2-methylphenoxy)acetic a;{2-Methyl-4-[4-Methyl-2-(4-trifluoroMethyl-phenyl)-thiazol-5-ylMethylsulfanyl]-phenoxy}-acetic acid
CAS:317318-70-0
MF:C21H18F3NO3S2
MW:453.5
EINECS:1592732-453-0
Product Categories:Inhibitors;Sarms;kl;Inhibitor;Antineoplastic;SARMs(Selective androgen receptor modulator);Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds;317318-70-0
Mol File:317318-70-0.mol
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GW-501516 Chemical Properties
Melting point 134-136°C
Boiling point 584.5±60.0 °C(Predicted)
density 1.42±0.1 g/cm3(Predicted)
storage temp. -20°C
solubility DMSO: soluble20mg/mL, clear
form powder
pka3.17±0.10(Predicted)
color white to beige
BRN 18515150
Stability:Light Sensitive
InChIInChI=1S/C21H18F3NO3S2/c1-12-9-16(7-8-17(12)28-10-19(26)27)29-11-18-13(2)25-20(30-18)14-3-5-15(6-4-14)21(22,23)24/h3-9H,10-11H2,1-2H3,(H,26,27)
InChIKeyYDBLKRPLXZNVNB-UHFFFAOYSA-N
SMILESC(O)(=O)COC1=CC=C(SCC2SC(C3=CC=C(C(F)(F)F)C=C3)=NC=2C)C=C1C
CAS DataBase Reference317318-70-0

Safety Information
WGK Germany 3
RTECS AI9105500
MSDS Information

GW-501516 Usage And Synthesis
DescriptionGW501516, also known as GW-1516 or cardarine and endurobol, is a peroxisome proliferator-activated receptor delta (PPAR-δ) agonist. Activation of the receptor will increase fat-burning capacity and muscle production, as it changes the body's fuel preference from glucose to lipids.
DescriptionPeroxisome proliferator-activated receptor δ (PPARδ) stimulation or over-expression in adipocytes leads to increased fatty acid oxidation, improved exercise tolerance, and resistance to obesity. GW 501516 is the first highly selective synthetic PPARδ agonist available. GW 501516 binds to human PPARδ with an IC50 value of 1 nM, and is at least 100-fold selective for PPARδ compared to PPARα and PPARγ. In obese primates, GW 501516 increases high density lipoprotein cholesterol and apolipoprotein A-1 specific reverse cholesterol transport. GW 501516 is therefore a model compound for a new type of obesity therapeutic, as well as a selective pharmacological tool for understanding lipid metabolism.
Chemical PropertiesWhite Solid
UsesAn experimental drug meant to control lipids and increase the level of HDL, or good cholesterol, in the bloodstream. A cell-permeable, thiazolyl compound that acts as a potent, high affinity, PPARd agonist. Exhibits selectivity for PPARd compared t
UsesGW501516 has been used to study its effect on mutation-driven colorectal tumorigenesis and tumor invasion using mouse model.
DefinitionChEBI: An aromatic ether that is phenoxyacetic acid in which the phenyl group is substituted at position 2 by a methyl group and at position 4 by a (1,3-thiazol-5-ylmethyl)sulfanediyl group, and in which the 1,3-thiazolyl group is substituted at positions 2 and 4 by p-trifluoromethylphenyl and methyl groups, respectively.
Biological ActivityGW 501516 is a potent and selective PPARδ agonist (EC50 = 1.2 nM). Displays <1000-fold selectivity over other PPAR subtypes. Increases ABC A1 transporter expression and induces apolipoprotein A1-mediated cholesterol efflux in vitro. Also increase serum HDL cholesterol and lowers small, dense LDL levels in obesity in vivo models.
Biochem/physiol ActionsPPARδ activation by GW501516, retards weight gain through fatty acid catabolism in adipose tissue and skeletal muscles. GW501516 causes an increase in the levels high-density lipoprotein cholesterol and apolipoprotein A (apoA) and reduction in the low density-lipoprotein cholesterol, apoB, and triglyceride.
Mechanism of actionGW501516 is a selective agonist (activator) of the PPARδ receptor. It displays high affinity (Ki = 1 nM) and potency (EC50 = 1 nM) for PPARδ with > 1,000 fold selectivity over PPARα and PPARγ.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.[31] 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).
storageStore at -20°C
References1) Oliver?et al.?(2001),?A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport; Proc. Natl. Acad. Sci. USA,?98?5306 2) Ito?et al.?(2012),?A PML-PPAR-δ pathway for fatty acid oxidation regulates hematopoietic stem cell maintenance; Nat. Med.,?18?1350 3) Barroso?et al. (2011), The PPARβ/δ activator GW501516 prevents the down-regulation of AMPK caused by a high-fat diet in liver and amplifies the PGC-1α-Lipin 1-PPARα pathway leading to increased fatty acid oxidation. Endocrinology,?152?1848 4) Okazaki?et al.?(2010),?PPAR beta/delta regulates the human SIRT1 gene transcription via Sp1; Endocr. J.,?57?403 5) Narkar?et al.?(2008),?AMPK and PPARdelta agonists are exercise mimetics; Cell,?134?405




































Company Profile Introduction

Shandong Huisheng Import & Export Co., Ltd. is located in Jinan city, Shandong Province, is a collection of domestic trade, international trade in one of the diversified services company. Our goal is to provide customers with high quality solutions and one-stop purchasing experience. At present, the company business scope involves five areas: Organic chemical raw materials, inorganic chemical raw materials, fine chemical raw materials, dangerous chemicals and green environmental protection chemical technology project promotion, and we has also established good relations of cooperation with several well-known enterprises and won the strong support of extensive trust from the new and old customers. Products are widely used in automobile, household appliances, office supplies, mobile phone accessories, routers, food, medical and other fields. At present, our business covers 30 countries, and our customers mainly come from Australia, New Zealand, Canada, Germany, France, Poland, South Korea, Russia, Bangladesh, Vietnam, Kazakhstan, India, Ghana, Nigeria, South Africa, Egypt and other more than 30 countries. The company has a sound quality management system and advanced professional equipment, with a positive attitude to meet the changing needs of customers. We take "quality products, quality service, competitive price, timely delivery" as the purpose, looking forward to greater cooperation with overseas customers on the basis of mutual benefit. Our company provides a wide range of products to meet your various needs. Since its inception, the company has always adhered to the "quality first, customer first, reputation first" business policy, wholeheartedly meet the potential needs of our customers. Under the irresistible situation of economic globalization, our company is willing to cooperate sincerely with enterprises around the world to achieve a win-win situation.

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