Free shipping on all orders over $ 500

GW501516

Cat. No. M3658
GW501516 Structure
Synonym:

GSK-516, GW1516

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 50  USD50 In stock
5mg USD 40  USD40 In stock
10mg USD 70  USD70 In stock
50mg USD 170  USD170 In stock
100mg USD 240  USD240 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

GW501516 (GSK-516, GW1516) is a potent and highly selective PPARβ/δ agonist, with EC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ. The PPARβ/δ agonist GW501516 inhibited the increase caused by TNF-α in the mRNA levels of the NF-κB target genes interleukin 8 (IL-8), TNF-α and thymic stromal lymphopoietin (TSLP). GW501516 exhibited agonist effects with EC(50) values of 560 and 55 nM against PPARα and PPARδ, respectively, in a luciferase assay. Moreover, GW501516 also exhibited potent ability to induce oleic acid oxidation in a human myotube cell assay with EC(50)=3.7 nM. In contrast, GW501516 treatment decreased TNF-α-induced p65 acetylation. GW501516 increased AMPK phosphorylation and the subsequent p300 phosphorylation, leading to a marked reduction in the association between p65 and this transcriptional co-activator.

Customer Product Validations & Biological Datas
Source Oncotarget (2017). Figure 1. GW501516
Method migration assay
Cell Lines MDA-MB-231, MDA-MB-435, and ZR-75-1 cells
Concentrations 100 nM
Incubation Time 48 h
Results Consistent with the results in MDA-MB-231 cells, the migration of other high metastatic human breast cancer cell lines MDA-MB-435 and ZR-75-1 was dose-dependently inhibited in the presence of GW501516
Chemical Information
Molecular Weight 453.5
Formula C21H18F3NO3S2
CAS Number 317318-70-0
Solubility (25°C) DMSO 47 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Lu T, et al. Diabetes. Reactive oxygen species signaling facilitates FOXO-3a/FBXO-dependent vascular BK channel β1 subunit degradation in diabetic mice.

[2] Iwaisako K, et al. Proc Natl Acad Sci U S A. Protection from liver fibrosis by a peroxisome proliferator-activated receptor δ agonist.

[3] Ciocoiu CC, et al. Bioorg Med Chem. Synthesis, molecular modeling studies and biological evaluation of fluorine substituted analogs of GW 501516.

[4] Barroso E, et al. Biochem Pharmacol. The peroxisome proliferator-activated receptor β/δ (PPARβ/δ) agonist GW501516 prevents TNF-α-induced NF-κB activation in human HaCaT cells by reducing p65 acetylation through AMPK and SIRT1.

Related PPAR Products
DSO-5a

DSO-5a is a potent, selective, orally active BB3 agonist.

Carfloglitazar sodium

Carfloglitazar sodium is a dual agonist of the pan peroxisome proliferator-activated receptor (PPARα/γ) with EC50 values of 1.2, 0.08, and 1.7 μM for PPARα, PPARγ, and PPARδ, respectively.It can be used in studies related to nonalcoholic steatohepatitis (NASH).

Seladelpar

Seladelpar is a potent, orally active, specific PPAR-δ agonist with an EC50 of 2 nM.

4'-O-Methylhonokiol

4-O-Methyl honokiol is a natural neolignan isolated from Magnolia officinalis, acts as a PPARγ agonist, and inhibtis NF-κB activity, used for cancer and inflammation research.

3-Phenyl-2-propen-1-ol

trans-Cinnamyl alcohol is a trans-isomer of Cinnamyl alcohol.

  Catalog
Abmole Inhibitor Catalog




Keywords: GW501516, GSK-516, GW1516 supplier, PPAR, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.