CAY10786 (GPR52 antagonist Comp-43) is a highly potent and specific GPR52 antagonist with IC50 of 0.63 uM.
Comp-43 showed no effects on the cAMP elevation or calcium response stimulated by other GPCRs (β2AR, GCGR, GLP-1R, CCR5, α-1D adrenergic receptor, and dopamine D2 receptor (DRD2).
Comp-43 reduces mHTT levels by targeting GPR52 and promotes survival of mouse primary striatal neurons.
Comp-43 not only reduces mHTT levels but also rescues Huntington's disease (HD)-related phenotypes in HdhQ140 mice.
Physicochemical Properties
M.Wt
242.336
Formula
C15H14OS
Appearance
Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO (2.4 mg/mL)
Chemical Name/SMILES
(2E)-5-phenyl-1-(2-thienyl)-2-penten-1-one
References
1. Hidetoshi Komatsu. J Med Chem. 2021 Jan 28;64(2):938-940.
2. Congcong Wang, et al. J Med Chem. 2021 Jan 28;64(2):941-957.
