GSK 3787

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Cat.No. 3961 - GSK 3787 | C15H12ClF3N2O3S | CAS No. 188591-46-0
Description: Potent and selective PPARδ antagonist
Chemical Name: 4-Chloro-N-[2-[[5-(trifluoromethyl)-2-pyridinyl]sulfonyl]ethyl]benzamide
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (3)

Biological Activity

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

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

Technical Data

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

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

Preparing Stock Solutions

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.

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

Certificate of Analysis / Product Datasheet
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References

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


If you know of a relevant reference for GSK 3787, please let us know.

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View all PPARδ Antagonists

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

1 Citation for GSK 3787

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

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


Do you know of a great paper that uses GSK 3787 from Tocris? Please let us know.

Reviews for GSK 3787

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Literature in this Area

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