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516567

Sigma-Aldrich

PPARβ/δ Antagonist, GSK3787

The PPARβ/δAntagonist II, PT-S58, also referenced under CAS 188591-46-0, controls the biological activity of PPARβ/δ. This small molecule/inhibitor is primarily used for Biochemicals applications.

Synonym(s):

PPARβ/δ Antagonist, GSK3787, 4-Chloro-N-(2-((5-trifluoromethyl)-2-pyridyl)sulfonyl)ethyl)benzamide, PPARβ Antagonist I, PPARδ Antagonist I

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100 μG
$513.00

$513.00


Estimated to ship onMarch 23, 2025


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100 μG
$513.00

About This Item

Empirical Formula (Hill Notation):
C15H12ClF3N2O3S
CAS Number:
Molecular Weight:
392.78
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77

$513.00


Estimated to ship onMarch 23, 2025


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Quality Level

assay

≥99% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 50 mg/mL, clear, colorless

shipped in

ambient

storage temp.

2-8°C

SMILES string

FC(F)(F)c1cnc(cc1)[S](=O)(=O)CCNC(=O)c2ccc(cc2)Cl

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MPHL20CF3MPVL20CL3MPVL20CF3
technique(s)

bioburden reduction: suitable

technique(s)

bioburden reduction: suitable

technique(s)

sterile filtration: suitable

technique(s)

sterile filtration: suitable

product line

Millipak® 200

product line

Millipak® 200

product line

Millipak® 200

product line

Millipak® 200

filtration area

1000 cm2

filtration area

1000 cm2

filtration area

1000 cm2

filtration area

1000 cm2

sterility

irradiated, non-sterile

sterility

irradiated, non-sterile

sterility

irradiated, non-sterile

sterility

irradiated, non-sterile

material

PVDF , polycarbonate , PVDF vent cap, polycarbonate support

material

PVDF , PVDF vent cap, polycarbonate , polycarbonate support

material

PVDF , PVDF vent cap, polycarbonate , polycarbonate support

material

PVDF , PVDF vent cap, polycarbonate , polycarbonate support

General description

A cell-permeable and orally available pyridylsulfone compound that acts as a selective, high affinity PPARβ (PPARδ) ligand (IC50 in PPAR ligand displacement assays = 200 nM against human PPARβ and >10 µM against PPARα or PPARγ) and effectively antagonizes agonist-induced, but not basal, PPARβ transcription activity both in cultures in vitro (IC50 = 126 nM against 2 nM GW501516-induced reporter transcription in CV-1 cells) and in mice in vivo (82% and 71% inhibition of 10 mg/kg GW0742-induced Adrp and Angptl4 mRNA upregulation, respectively, in colon epithelium by 10 mg/kg GSK3787; p.o.) by covalently modifying PPARβ at Cys249. GSK3787 is also shown to exhibit weak agonistic activity toward PPARγ (1.2-fold increase above basal level by 1 µM GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 µM GW1929 in the presence or absence of 1 µM GSK3787, respectively).
A cell-permeable pyridylsulfone that acts as a selective, high affinity PPARβ (PPARδ) ligand (IC50 in PPAR ligand displacement assays = 200 nM against human PPARβ and >10 µM against PPARα or PPARγ) and effectively antagonizes agonist-induced, but not basal, PPARβ transcription activity both in cultures in vitro (IC50 = 126 nM in CV-1 cells) and in mice in vivo (82% and 71% inhibition of 10 mg/kg GW0742-induced Adrp and Angptl4 mRNA upregulation, respectively, in colon epithelium; 10 mg/kg GSK3787; p.o.) by covalently modifying PPARβ at Cys249. GSK3787 is also shown to exhibit weak agonistic activity toward PPARγ (1.2-fold increase above basal level by 1 µM GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 µM GW1929 in the presence or absence of 1 µM GSK3787, respectively).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Palkar, P.S., et al. 2010. Mol. Pharmacol.78, 419.
Shearer, B,G., et al. 2010. J. Med. Chem.53, 1857.

Legal Information

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

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


Certificates of Analysis (COA)

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