GW-501516
- CAS No.
- 317318-70-0
- Chemical Name:
- GW-501516
- Synonyms
- CARDARINE;GW 1516;2-[2-Methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]acetic Acid;ENDUROBOL;CS-788;GSK-516;CARDAROL;GW-501615;Cardrarine;SARMS GW501516
- CBNumber:
- CB31476045
- Molecular Formula:
- C21H18F3NO3S2
- Molecular Weight:
- 453.5
- MDL Number:
- MFCD09033000
- MOL File:
- 317318-70-0.mol
- MSDS File:
- SDS
| 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 |
| pka | 3.17±0.10(Predicted) |
| color | white to beige |
| BRN | 18515150 |
| Stability | Light Sensitive |
| InChI | InChI=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) |
| InChIKey | YDBLKRPLXZNVNB-UHFFFAOYSA-N |
| SMILES | C(O)(=O)COC1=CC=C(SCC2SC(C3=CC=C(C(F)(F)F)C=C3)=NC=2C)C=C1C |
| CAS DataBase Reference | 317318-70-0 |
| FDA UNII | 7I2HA1NU22 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H315-H319-H335 | |||||||||
| Precautionary statements | P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P321-P362+P364-P332+P313-P337+P313-P403+P233-P405-P501 | |||||||||
| WGK Germany | 3 | |||||||||
| RTECS | AI9105500 | |||||||||
| NFPA 704 |
|
GW-501516 price More Price(44)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML1491 | {2-Methyl-4-{{4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl}methylthio}phenoxy}acetic acid ≥98% (HPLC) | 317318-70-0 | 5mg | $111 | 2024-03-01 | Buy |
| Sigma-Aldrich | 43732 | {2-Methyl-4-{{4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl}methylthio}phenoxy}acetic acid analytical standard | 317318-70-0 | 25mg | $281 | 2022-05-15 | Buy |
| Cayman Chemical | 10004272 | GW 501516 ≥98% | 317318-70-0 | 1mg | $44 | 2024-03-01 | Buy |
| Cayman Chemical | 10004272 | GW 501516 ≥98% | 317318-70-0 | 5mg | $87 | 2024-03-01 | Buy |
| Sigma-Aldrich | SML1491 | {2-Methyl-4-{{4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl}methylthio}phenoxy}acetic acid ≥98% (HPLC) | 317318-70-0 | 25mg | $449 | 2024-03-01 | Buy |
GW-501516 Chemical Properties,Uses,Production
Description
Peroxisome proliferator-
Description
GW501516, 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.
Chemical Properties
White Solid
History
GW501516, also known as Cardarine, was originally discovered in the early 1990s during a research collaboration between two large pharmaceutical companies. The initial proposed use was for the treatment of hyperlipidemia (elevated fats in the blood), though later studies looked at its effectiveness for treating obesity, diabetes, and cardiovascular disease.
Uses
GW501516 has been used to study its effect on mutation-driven colorectal tumorigenesis and tumor invasion using mouse model.
Uses
An 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
Definition
ChEBI: 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.
General Description
GW501516 is the most selective and potent PPARβ (EC50=1.1nM) agonist that has been demonstrated to be 1,000-fold more selective in comparison to existing subtypes. It can regulate expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells and has been shown to block insulin resistance and fatty acid-induced nuclear factor-κB (NF-κB) activation.
Biological Activity
GW 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 Actions
PPARδ 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 action
GW501516 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).
storage
Store at -20°C
References
1) 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
GW-501516 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Longyu Biotechnology Co., Ltd. | +8619521488211 | info@longyupharma.com | China | 2524 | 58 |
| Changzhou Xuanming Pharmaceutical Technology Co., Ltd. | +8615995072465 | sales@xuanmingchem.com | China | 914 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| Wuhan Cell Pharmaceutical Co., Ltd | +86-13129979210 +86-13129979210 | sales@cellwh.com | China | 376 | 58 |
| hebei hongtan Biotechnology Co., Ltd | +86-86-1913198-3935 +8617331935328 | sales03@chemcn.cn | China | 970 | 58 |
| CONTIDE BIOTECH CO.,LTD | +852-7026-8763 +85253358525 | amy@healthtide-api.com | China | 554 | 58 |
| Shanghai Getian Industrial Co., LTD | +86-15373193816 +86-15373193816 | mike@ge-tian.com | China | 269 | 58 |
| Hebei Yanxi Chemical Co., Ltd. | +8617531190177 | peter@yan-xi.com | China | 5858 | 58 |
| Firsky International Trade (Wuhan) Co., Ltd | +8615387054039 | admin@firsky-cn.com | China | 427 | 58 |
| qingdao future trading Co., Ltd | +86-13335044410 +86-13335044410 | cui56813@163.com | China | 110 | 58 |
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- Sep 27，2023
- Synthesis and Application of GW-501516
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View Lastest Price from GW-501516 manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2024-11-05 | GW-501516/Cardarine 10mg Tablets
317318-70-0
|
US $0.00-0.00 / Bottle | 1Bottle | 99% | 20000 | Shandong Huizhihan Supply Chain Co., Ltd | |
 |
2024-11-05 | GW-501516?/?Cardarine
317318-70-0
|
US $30.00 / g | 10g | 99% | 1000kg | hebei hongtan Biotechnology Co., Ltd | |
 |
2024-11-05 | GW-501516
317318-70-0
|
US $0.00 / G | 1G | 99% | 20 | CONTIDE BIOTECH CO.,LTD |
-
- GW-501516/Cardarine 10mg Tablets
317318-70-0
- US $0.00-0.00 / Bottle
- 99%
- Shandong Huizhihan Supply Chain Co., Ltd
-
- GW-501516?/?Cardarine
317318-70-0
- US $30.00 / g
- 99%
- hebei hongtan Biotechnology Co., Ltd
-
- GW-501516
317318-70-0
- US $0.00 / G
- 99%
- CONTIDE BIOTECH CO.,LTD