GW9662_22978-25-2_DataSheet_MedChemExpress
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Product Name:
GW9662CAS No.:
22978-25-2Cat. No.:
HY-16578Product Data Sheet MWt:
276.68Formula:
C13H9ClN2O3Purity :>98%
Solubility:
DMSO 25 mg/ml Ethanol 25 mg/ml
Mechanisms:Biological Activity:
GW9662 is a selective PPAR antagonist for PPAR γ with IC50 of 3.3 nM, with ~10 and ~1000-fold
Pathways:NF-KB; Target:PPAR
Pathways:Cell Cycle/DNA Damage; Target:PPAR
functional selectivity in cells against PPAR α and PPAR δ, respectively.
IC50 Value: 3.3 nM(for PPAR γ); 32 nM(for PPAR α); 2 uM(for PPAR δ)
Target: PPAR γin vitro: GW9662 is a selective PPAR γ antagonist (IC50 values are 3.3, 32 and 2000 nM for PPAR γ,PPAR α and PPAR δ respectively). GW9662 blocks the inhibition of osteoclast formation induced by IL-4 in the low micromolar range (1-2 μM), therefore is more potent than BADGE. PPAR γantagonist GW9662 may inhibit the foam-cell formations in atherosclerosis. GW9662 induces functional estrogen receptor in mouse mammary organ culture. Anticancer, inhibits growth of
human mammary tumor cell lines The induction of ER by GW9662including newer analogs may References:
[1]. Rajendra G. Mehta, Xinjian Peng, Sarbani Roy, et al. PPAR γ antagonist GW9662 induces functional estrogen receptor in mouse mammary organ culture: potential translational significance.Molecular and Cellular Biochemistry 2013372(12):249256human mammary tumor cell lines. The induction of ER α by GW9662, including newer analogs, may
permit use of anti-ER strategies to inhibit breast cancer in ER-patients.in vivo: ...
Molecular and Cellular Biochemistry. 2013, 372(1-2): 249-256.
[2]. Karen K Ryan, Bailing Li, Bernadette E Grayson, et al. A role for central nervous system PPAR-γ
in the regulation of energy balance. Nature Medicine, 2011,17, 623-626.[3]. Collino M, Patel NS, Lawrence KM, et al. The selective PPARgamma antagonist GW9662reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005
Aug;68(2):529-36.[4]. Seargent JM, Yates EA, Gill JH. GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation. Br J Pharmaco...
Caution: Not fully tested. For research purposes only
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