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Merck

516568

PPARβ/δ Inverse Agonist

The PPARβ/δ Inverse Agonist controls the biological activity of PPARβ/δ.

Synonym(s):

PPARβ/δ Inverse Agonist, methyl 3-(N-(4-(hexylamino)-2-methoxyphenyl)sulfamoyl)thiophene-2-carboxylate (ST247)

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About This Item

Empirical Formula (Hill Notation):
C19H26N2O5S2
Molecular Weight:
426.55
UNSPSC Code:
12352200

Product Name

PPARβ/δ Inverse Agonist, The PPARβ/δ Inverse Agonist controls the biological activity of PPARβ/δ.

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

yellow

solubility

DMSO: 100 mg/mL, clear, amber-yellow

shipped in

ambient

storage temp.

−20°C

Quality Level

100

Disclaimer

Toxicity: Standard Handling (A)

General description

A cell-permeable, diaryl sulfonamide inverse agonist that demonstrates selectivity for the ligand-binding domain of the PPAR β/δ receptor (IC50 = 93 nM). Enhances the interaction of the PPARβ/δ ligand-binding domain with the co-repressor, SMRT-ID2 (EC50 = 10 nM). Down-regulates the peroxisome proliferator response elements (PPREs)-driven target gene, ANGPTL4. Inhibits PPARβ/δ- specific agonist-induced transcriptional activity in human myofibroblasts and mouse thioglycollate-elicited peritoneal macrophages.

Other Notes

Naruhn, S., et al. 2011., Mol Pharmacol.80, 828.

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class

11 - Combustible Solids

wgk

WGK 3

Certificates of Analysis (COA)

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