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CAY10786

Chemical Structure : CAY10786

CAS No.: 1239987-91-7

CAY10786 (GPR52 antagonist Comp-43)

Catalog No.: PC-72128Not For Human Use, Lab Use Only.

CAY10786 (GPR52 antagonist Comp-43) is a highly potent and specific GPR52 antagonist with IC50 of 0.63 uM.

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Biological Activity

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.

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