Home / PPAR delta Receptor Antagonists / GSK 3787

GSK 3787

Catalog #: 3961
4 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
3961/10
3961/50
GSK 3787 | CAS No. 188591-46-0 | PPAR delta Receptor Antagonists
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Description: Potent and selective PPARδ antagonist

Chemical Name: 4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide

Purity: ≥99%

Product Details
Citations (4)
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Biological Activity

GSK 3787 is a potent and selective peroxisome proliferator-activated receptor δ (PPARδ) antagonist (pIC50 = 6.6). Displays no measurable affinity for PPARα or PPARγ in vitro (pIC50< 5).

Technical Data

M.Wt:
392.78
Formula:
C15H12ClF3N2O3S
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥99%
Storage:
Store at +4°C
CAS No:
188591-46-0

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. Telmisartan activates endothelial nitric oxide synthase via Ser1177 phosphorylation in vascular endothelial cells.
    Myojo, Masahiro, Nagata, Daisuke, Fujita, Daishi, Kiyosue, Arihiro, Takahashi, Masao, Satonaka, Hiroshi, Morishita, Yoshiyuk, Akimoto, Tetsu, Nagai, Ryozo, Komuro, Issei, Hirata, Yasunobu
    PLoS ONE, 2014;9(5):e96948.
  2. Identification and characterization of 4-chloro-N(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist.
    Shearer et al.
    J.Med.Chem., 2010;53:1857
  3. Cellular and pharmacological selectivity of the peroxisone proliferator-activated receptor-β/δ antagonist GSK3787.
    Palkar et al.
    Mol.Pharmacol., 2010;78:419

Product Datasheets

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Citations for GSK 3787

The citations listed below are publications that use Tocris products. Selected citations for GSK 3787 include:

4 Citations: Showing 1 - 4

  1. Nuclear receptor modulators inhibit osteosarcoma cell proliferation and tumour growth by regulating the mTOR signaling pathway.
    Authors: Ning Et al.
    Cell Death Dis  2023;14:51
  2. Peroxisome Proliferator-Activated Receptor Activation in Precision-Cut Bovine Liver Slices Reveals Novel Putative PPAR Targets in Periparturient Dairy Cows.
    Authors: Massimo Et al.
    Front Vet Sci  2022;9:931264
  3. The interplay between non-esterified fatty acids and bovine peroxisome proliferator-activated receptors: results of an in vitro hybrid approach.
    Authors: Sebastiano Et al.
    J Anim Sci Biotechnol  2020;11:91
  4. PPARδ signaling mediates the cytotoxicity of DHA in H9c2 cells.
    Authors: Samokhvalov Et al.
    Cell Cycle  2015;232:44105

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