GW501516
GW501516 is subtype-selective small-molecule agonist of peroxisome proliferator-activated receptor δ (PPARδ) with Ki value of 1.1nM [1].
GW501516 is discovered by combinatorial chemistry and structure-based drug design to use as an ideal chemical tool to study the function of the ubiquitously expressed PPARδ. In the cell-based transfection assay, it induces expression of a GAL4-responsive reporter gene with EC50 value of 1.2nM. GW501516 shows more than 1000-fold selective for PPARδ over other subtypes. PPARδ is expressed in many tissues that contribute to cholesterol flux, and is a RXR of partner. As an agonist of PPARδ, GW501516 is found to increase the expression of ABCA1 as well as the apoA1-specific cholesterol efflux. In primate model of human metabolic disease, GW501516 increases the level of HDLc and lowers the fasting triglycerides. GW501516 also produces fewer, yet larger, LDL and VLDL particles results in a less atherogenic lipid composition. Furthermore, GW501516 partially corrects the hyperinsulinemia in primates without adverse effects on glycemic control [1, 2].
References:
[1] Wei ZL, Kozikowski AP. A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta. J Org Chem. 2003 Nov 14;68(23):9116-8.
[2] Oliver WR Jr, 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. A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport. Proc Natl Acad Sci U S A. 2001 Apr 24;98(9):5306-11.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 453.5 |
Cas No. | 317318-70-0 |
Formula | C21H18F3NO3S2 |
Solubility | insoluble in H2O; ≥18.05 mg/mL in DMSO; ≥44.6 mg/mL in EtOH |
Chemical Name | 2-[2-methyl-4-[[4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl]methylsulfanyl]phenoxy]acetic acid |
SDF | Download SDF |
Canonical SMILES | CC1=C(C=CC(=C1)SCC2=C(N=C(S2)C3=CC=C(C=C3)C(F)(F)F)C)OCC(=O)O |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Cell experiment:[1] | |
Cell lines |
THP1 macrophages, 1BR3N human skin fibroblasts and FHS74 human intestinal cells |
Reaction Conditions |
100 nM GW501516 |
Applications |
In macrophages, fibroblasts, and intestinal cells, GW501516 increased expression of the reverse cholesterol transporter ATP-binding cassette A1 (ABCA1) and induced apolipoprotein A1-specific cholesterol efflux. These results suggest that GW501516 may promote cholesterol efflux from multiple tissues by increasing expression of the reverse cholesterol transporter ABCA1. |
Animal experiment:[2] | |
Animal models |
A rat model of non-alcoholic fatty liver disease induced by a high-fat diet |
Dosage form |
10 mg/kg Once daily by oral route for 4 weeks |
Applications |
After 4 weeks of treatment with GW501516, the hepatosomatic index was almost reduced to the level of the normal control group. In addition, a significant decrease in body mass index was observed in the rats that were treated with GW501516 for 4 weeks. GW501516 was found to alleviate non-alcoholic fatty liver disease by modulating glucose and fatty acid metabolic enzymes in a rat model. |
Note |
The technical data provided above is for reference only. |
References: 1. Oliver WR Jr, Shenk JL, Snaith MR, et al. A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport. Proceedings of the National Academy of Sciences of the United States of America, 2001, 98(9): 5306-5311. 2. Li X, Li J, Lu X, et al. Treatment with PPARδ agonist alleviates non-alcoholic fatty liver disease by modulating glucose and fatty acid metabolic enzymes in a rat model. International Journal of Molecular Medicine, 2015, 36(3): 767-775. |
Description | GW501516 is a selective and potent agonist of PPARβ with EC50 value of 1.1 nM. | |||||
Targets | PPARβ | |||||
IC50 | 1.1 nM (EC50) |
Quality Control & MSDS
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Chemical structure
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Related Biological Data
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