- GW-501516
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- $0.00 / 1KG
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2024-03-16
- CAS:
- Min. Order: 100g
- Purity: 98%+
- Supply Ability: 100kg
- GW-501516
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- $10.00 / 1mg
-
2024-03-08
- CAS:317318-70-0
- Min. Order: 1mg
- Purity: 99%
- Supply Ability: 1000g
- GW-501516
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- $1.00 / 1g
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2024-02-22
- CAS:
- Min. Order: 5g
- Purity: 99%min
- Supply Ability: 1000kgs/month
Related articles - Uses and Mode of action of GW501516
- GW501516 (also known as GW-501,516, GW1516, GSK-516, Cardarine) is a PPARδ receptor agonist that was invented in a collaborati....
- Aug 11，2022
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| | GW501516 Basic information |
| Product Name: | GW501516 | | Synonyms: | 2-METHYL-4-((4-METHYL-2-(4-TRIFLUOROMETHYLPHENYL)-1,3-THIAZOL-5-YL)-METHYLSULFANYL)PHENOXY-ACETIC ACID;GW501516 | | CAS: | | | MF: | C21H20F3NO3S2 | | MW: | 455.51 | | EINECS: | | | Product Categories: | | | Mol File: | Mol File |  |
| | GW501516 Chemical Properties |
| Melting point | 134 - 144°C | | storage temp. | Refrigerator | | solubility | DMSO (Slightly), Methanol (Slightly) | | form | Solid | | color | White to Pale Yellow |
| | GW501516 Usage And Synthesis |
| 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, PPARδ agonist. Exhibits selectivity for PPARδ compared to PPARα and PPARγ. Does not exibit any activity against other nuclear or non-nuclear receptors. Reported to increase cholesterol efflux and ABAC1 expression in macrophages, fibroblasts, and intestinal cells. GW 501516 has been found to enhance endurance in mice without any training. | | Biological Activity | GW 501516 is shown to be the most potent and selective PPARα agonists known with an EC50
of 1.1 nM against PPARα and 1000-fold selectivity over the other human
subtypes, PPARα and-γ. GW 501516 exerts anti-inflammatory effects in
mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits
palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a
dose-dependent manner. | | Synthesis | Add Cs2CO3
(3.25 g, 10.0 mmol), followed by the chloromethylthiazole (2.60 g) to a
stirred solution of 4-mercapto-2-methylphenol (1.40 g) in CH3CN (80
mL). Stir the reaction mixture at room temperature for 4 hours. Add Cs2CO3
(4.89 g, 15.0 mmol), followed by methyl bromoacetate (1.23 mL, 13.0
mmol) to the mixture. Stir the reaction mixture at room temperature for
another 5 hours. Pour the mixture into water. Extract the mixture with
EtOAc (3 x 100 mL). Combine the organic layers. Wash the organic layers
with brine. Dry the organic layers (Na2SO4). Concentrate the organic layers. Purify the residue by column chromatography on silica gel with hexane/ ethyl acetate (5:1). 1H NMR (CDCl3)
δ7.97 (d, 2H, J= 8.4 Hz), 7.65 (d, 2H, J= 8.4 Hz), 7.21 (d, 1H, J= 2.4
Hz), 7.13 (dd, 1H, J= 8.4, 2.4 Hz), 6.58 (d, 1H, J= 8.4 Hz), 4.63 (s,
2H), 4.11 (s, 2H), 3.78 (s, 3H), 2.24 (s, 3H), 2.20 (s, 3H). 13C NMR (CDCl3)
δ169.2, 163.0, 156.3, 151.3, 136.8, 136.1, 132.1, 131.2 (q, J= 32 Hz),
130.6, 128.4, 126.3, 125.8 (q, J= 4 Hz), 125.3, 122.1, 111.4, 65.4,
52.2, 32.4, 16.1, 14.8. 19F NMR (CDCl3) δ115.5 (s).
Fig. The synthetic step 1 of GW-501516 |
| | GW501516 Preparation Products And Raw materials |
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