| Bioactivity | 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]. | ||||||||||||
| Target | IC50: 0.63 μM (GPR52) | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | GPR52 antagonist-1 | ||||||||||||
| CAS | 1239987-91-7 | ||||||||||||
| Formula | C15H14OS | ||||||||||||
| Molar Mass | 242.34 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| 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. |