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Product Description
– GW9662-d5 is the deuterium labeled GW9662. GW9662 is a potent and selective PPARγ antagonist with an IC50 of 3.3 nM, showing 10 and 1000-fold selectivity over PPARα and PPARδ, respectively[1][2].
Web ID
– HY-16578S
Shipping
– Room temperature
Molecular Formula
– C13H4D5ClN2O3
References
– [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. |[2]Seargent JM, et al. GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumor cells and promotes the anticancer effects of the PPARgamma agonist BRL 49653, independently of PPARgamma activation. Br J Pharmacol. 2004 Dec;143(8):933-7.|[3]Collino M, et al. The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005 Aug;68(2):529-36.|[4]Leesnitzer LM, et al. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Biochemistry. 2002 May 28;41(21):6640-50.|[5]Sato K, et al. PPARγ antagonist attenuates mouse immune-mediated bone marrow failure by inhibition of T cell function.Haematologica. 2016 Jan;101(1):57-67.
CAS Number
– 2117730-84-2
Molecular Weight
– 281.71
SMILES
– ClC1=CC=C(C=C1C(NC2=C(C([2H])=C(C([2H])=C2[2H])[2H])[2H])=O)[N+]([O-])=O
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Isotope-Labeled Compounds;PPAR
Pathway
– Cell Cycle/DNA Damage;Others;Vitamin D Related/Nuclear Receptor
Product type
– Isotope-Labeled Compounds
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