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GSK 3787

Cat. No. M2033
GSK 3787 Structure
Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 380 In stock
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Quality Control
Biological Activity

GSK3787 is a potent and selective PPARbeta/delta antagonist. GSK3787 displays no measurable affinity for PPARα or PPARγ in vitro (pIC50< 5). GSK3787 has been shown to antagonize the induction of PPARδ-regulated target genes in skeletal muscle cells. In addition, GSK 3787 acts in a dual role as a weak agonist and antagonist towards PPARγ. In vivo and in vitro analysis indicates that the efficacy of GSK3787 to modulate PPARgamma activity is markedly lower than the efficacy of GSK3787 to act as a PPARbeta/delta antagonist. GSK3787 antagonized GW0742-induced expression of Angptl4 in mouse fibroblasts, mouse keratinocytes, and human cancer cell lines.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 392.78
Formula C15H12ClF3N2O3S
CAS Number 188591-46-0
Purity 98.64%
Solubility DMSO
Storage at -20°C
References

Cellular and pharmacological selectivity of the peroxisome proliferator-activated receptor-beta/delta antagonist GSK3787.
Palkar PS, et al. Mol Pharmacol. 2010 Sep;78(3):419-30. PMID: 20516370.

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 BG, et al. J Med Chem. 2010 Feb 25;53(4):1857-61. PMID: 20128594.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK 3787 supplier, PPAR, inhibitors

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