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Submit ReviewGSK 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).
GSK 3787 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 39.28 | 100 |
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 |
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.
Keywords: GSK 3787, GSK 3787 supplier, GSK3787, peroxisome, proliferator-activated, receptor, PPARd, PPARdelta, PPARδ, antagonists, Receptors, 3961, Tocris Bioscience
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
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
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
Do you know of a great paper that uses GSK 3787 from Tocris? Please let us know.
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