A GPR52 antagonist
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GPR52 Comp-43

Item No. 33564

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-5-phenyl-1-(2-thienyl)-2-penten-1-one
CAS Number
1239987-91-7
Synonyms
  • GPR52-IN-43
Molecular Formula
C15H14OS
Formula Weight
242.3
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
Chloroform: 10 mg/ml
λmax
270 nm
SMILES
O=C(C1=CC=CS1)/C=C/CCC2=CC=CC=C2
InChi Code
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+
InChi Key
XUIAIACHIPOOHR-BJMVGYQFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    5 mg

    $70

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    10 mg

    $118

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    25 mg

    $256

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    50 mg

    $477

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    Product Description

    GPR52 comp-43 is an antagonist of G protein-coupled receptor 52 (GPR52; IC50 = 0.63 µM).1 It reduces mutant huntingtin (mHTT) protein levels in STHdhQ7/Q111 cells, a heterozygous in vitro model of Huntington's disease, in a concentration-dependent manner. GPR52 comp-43 (3 µM) reduces apoptosis induced by growth factor deprivation in primary striatal neurons isolated from the heterozygous HdhQ7/Q140 mouse model of Huntington's disease. It decreases striatal levels of soluble and insoluble mHTT, as well as increases the latency to fall in the rotarod test, in the homozygous HdhQ140 mouse model of Huntington's disease, when administered at a dose of 5 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, C., Zhang, Y.-F., Guo, S., et al. GPR52 antagonist reduces huntingtin levels and ameliorates Huntington’s disease-related phenotypes. J. Med. Chem. 64(2), 941-957 (2021).