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GW-9662 | PPAR gamma antagonist

CAS:
22978-25-2
Catalog Number:
10-2622
Activity:
PPAR gamma antagonist
Chemical Name:
2-Chloro-5-nitrobenzanilide
Molecular Weight:
276.68
Molecular Formula:
C13H9ClN2O3
Solubility:
Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 10 mg/ml).
Physical Properties:
White or off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT

GW-9662 (22978-25-2) is a selective PPARγ antagonist (IC50 = 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively).1 Blocks the inhibition of osteoclast formation induced by IL-4 (1-2 μM).2 Displays anticancer activity inhibits growth of human mammary tumor cell lines.3 GW-9662 is a useful tool for dissecting the involvement of PPARγ in cellular physiology.4,5

References/Citations:

1) Leesnitzer et al. (2002), Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662; Biochemistry, 41 6640
2) Bendixen et al. (2001), IL-4 inhibits osteoclast formation through a direct action on osteoclast precursors via peroxisome proliferator-activated receptor gamma 1; Proc. Natl. Acad. Sci. USA, 98 2443
3) Seargent et al. (2004), GW9662, a potent antagonist of PPARgamma inhibits growth of breast cancer tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation; Br. J. Pharmacol., 143 933
4) Cheng et al. (2014), β-Caryophyllene Ameliorates the Alzheimer-Like Phenotype in APP/PS1 Mice through CB2 Receptor Activation and the PPARγ Pathway; Pharmacology, 94 1
5) Liu et al. (2014), Curcumin protects neurons against oxygen-glucose deprivation/reoxygenation-induced injury through activation of peroxisome proliferator-activated-γ function; J. Neuro. Sci. Res., 92 1549

GW-9662 | PPAR gamma antagonist is also available in the Cellular Metabolism Library.
CAS:
22978-25-2
Catalog Number:
10-2622
Activity:
PPAR gamma antagonist
Chemical Name:
2-Chloro-5-nitrobenzanilide
Molecular Weight:
276.68
Molecular Formula:
C13H9ClN2O3
Solubility:
Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 10 mg/ml).
Physical Properties:
White or off-white solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

Product Data Sheet:

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