GPR52 antagonist-1

• CAT Number: I025081
• CAS Number: 1239987-91-7
• Molecular Formula: C15H14OS
• Molecular Weight: 242.34
• Purity: ≥95%
• Synonyms: (E)-5-phenyl-1-thiophen-2-ylpent-2-en-1-one
• InChI: InChI=1S/C15H14OS/c16-14(15-11-6-12-17-15)10-5-4-9-13-7-2-1-3-8-13/h1-3,5-8,10-12H,4,9H2/b10-5+
• InChIKey: XUIAIACHIPOOHR-BJMVGYQFSA-N
• SMILES: C1=CC=C(C=C1)CCC=CC(=O)C2=CC=CS2

GPR52 antagonist-1 (Compound 43) is a GPR52 antagonist with an IC50 of 0.63 μM. GPR52 antagonist-1 reduces mHTT (mutant huntingtin protein) levels by targeting GPR52 and promotes survival of mouse primary striatal neurons[1].
GPR52 antagonist-1 (Compound 43) (5 mg/kg; i.p.; once a day for 4 weeks) reduces mHTT levels and rescues HD-related phenotypes in HdhQ140 mice[1].

Reference

[1]. Wang C, et al. GPR52 Antagonist Reduces Huntingtin Levels and Ameliorates Huntington’s Disease-Related Phenotypes. J Med Chem. 2021 Jan 28;64(2):941-957.
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