GPR52 antagonist E7 | GPR52 antagonist

Chemical Structure : GPR52 antagonist E7

GPR52 antagonist E7 (AD31E7)

Catalog No.: PC-72129Not For Human Use, Lab Use Only.

GPR52 antagonist E7 is a novel Gpr52 antagonist, shows significant inhibitory effect on WO-459 (100 nM)-induced cAMP elevation in HEK293/GPR52 cells with IC50 of 12.0 uM.

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Biological Activity

GPR52 antagonist E7 is a novel Gpr52 antagonist, shows significant inhibitory effect on WO-459 (100 nM)-induced cAMP elevation in HEK293/GPR52 cells with IC50 of 12.0 uM.
GPR52 antagonist E7 did not block cAMP elevation induced by Gαs-coupled GPCRs, including β2AR, GCGR and GLP-1R.
GPR52 antagonist E7 reduces mutant HTT levels and rescues Huntington's disease-associated phenotypes in cellular and mouse models.
GPR52 antagonist E7 acts as an tntracellular covalent ligand of orphan receptor GPR52.

Physicochemical Properties

M.Wt	358.39
Formula	C20H22O6
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
Chemical Name/SMILES	(3aR,4S,6Z,11E,12aR)-11-methyl-3-methylene-2,7-dioxo-2,3,3a,4,5,9,10,12a-octahydro-7H-6,9-(metheno)furo[2,3-f][1]oxacycloundecin-4-yl (Z)-2-methylbut-2-enoate

References

1. Song H, et al. Brain. 2018 Jun 1;141(6):1782-1798.

2. Ma M, et al. ACS Chem Biol. 2020 Dec 18;15(12):3275-3284.

GPR52 antagonist E7 (AD31E7)

Biological Activity

Physicochemical Properties

References

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