GSK 3787

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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% (HPLC)
Datasheet
Citations (4)
Reviews

Biological Activity for GSK 3787

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).

Compound Libraries for GSK 3787

GSK 3787 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for GSK 3787

M. Wt 392.78
Formula C15H12ClF3N2O3S
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 188591-46-0
PubChem ID 2800647
InChI Key JFUIMTGOQCQTPF-UHFFFAOYSA-N
Smiles O=C(C2=CC=C(Cl)C=C2)NCCS(C1=CC=C(C(F)(F)F)C=N1)(=O)=O

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.

Solubility Data for GSK 3787

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 39.28 100

Preparing Stock Solutions for GSK 3787

The following data is based on the product molecular weight 392.78. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.55 mL 12.73 mL 25.46 mL
5 mM 0.51 mL 2.55 mL 5.09 mL
10 mM 0.25 mL 1.27 mL 2.55 mL
50 mM 0.05 mL 0.25 mL 0.51 mL

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Product Datasheets for GSK 3787

Certificate of Analysis / Product Datasheet
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References for GSK 3787

References are publications that support the biological activity of the product.

Shearer et al (2010) 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. J.Med.Chem. 53 1857 PMID: 20128594

Palkar et al (2010) Cellular and pharmacological selectivity of the peroxisone proliferator-activated receptor-β/δ antagonist GSK3787. Mol.Pharmacol. 78 419 PMID: 20516370


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Keywords: GSK 3787, GSK 3787 supplier, GSK3787, peroxisome, proliferator-activated, receptor, PPARd, PPARdelta, PPARδ, antagonists, Receptors, 3961, Tocris Bioscience

4 Citations for GSK 3787

Citations are publications that use Tocris products. Selected citations for GSK 3787 include:

Ning et al (2023) Nuclear receptor modulators inhibit osteosarcoma cell proliferation and tumour growth by regulating the mTOR signaling pathway. Cell Death Dis 14 51 PMID: 36681687

Sebastiano et al (2020) The interplay between non-esterified fatty acids and bovine peroxisome proliferator-activated receptors: results of an in vitro hybrid approach. J Anim Sci Biotechnol 11 91 PMID: 32793344

Massimo et al (2022) Peroxisome Proliferator-Activated Receptor Activation in Precision-Cut Bovine Liver Slices Reveals Novel Putative PPAR Targets in Periparturient Dairy Cows. Front Vet Sci 9 931264 PMID: 35903133

Samokhvalov et al (2015) PPARδ signaling mediates the cytotoxicity of DHA in H9c2 cells. Cell Cycle 232 44105 PMID: 25300478


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