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GPR52 Comp-43

Cat. No. 7445 Submit a Review Datasheet / COA / SDS
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Description: GPR52 receptor antagonist
Chemical Name: (2E)-5-Phenyl-1-(2-thienyl)-2-penten-1-one
Purity: ≥98% (HPLC)
Datasheet
Citations
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for GPR52 Comp-43

GPR52 Comp-43 is a GPR52 receptor antagonist (IC50 = 0.63 μM). The use of GPR52 Comp-43 in animal models of Huntington's Disease leads to degradation and reduction of soluble and aggregated mutant huntingtin protein in the striatum. It also reduces neuronal loss, promotes neuronal survival and improves motor functions in vivo. GPR52 Comp-43 is active in vitro and brain penetrant.

Technical Data for GPR52 Comp-43

M. Wt 242.34
Formula C15H14OS
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 1239987-91-7
PubChem ID 156588927
InChI Key XUIAIACHIPOOHR-BJMVGYQFSA-N
Smiles O=C(C1=CC=CS1)/C=C/CCC2=CC=CC=C2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GPR52 Comp-43

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 24.23 100
ethanol 24.23 100

Preparing Stock Solutions for GPR52 Comp-43

The following data is based on the product molecular weight 242.34. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.13 mL 20.63 mL 41.26 mL
5 mM 0.83 mL 4.13 mL 8.25 mL
10 mM 0.41 mL 2.06 mL 4.13 mL
50 mM 0.08 mL 0.41 mL 0.83 mL

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Product Datasheets for GPR52 Comp-43

Certificate of Analysis / Product Datasheet
Safety Datasheet

References for GPR52 Comp-43

References are publications that support the biological activity of the product.

Wang et al (2021) GPR52 antagonist reduces huntingtin levels and ameliorates Huntington's disease-related phenotypes. J.Med.Chem. 64 941 PMID: 33185430

Komatsu (2021) Discovery of the first druggable GPR52 antagonist to treat Huntington's disease. J.Med.Chem. 64 938 PMID: 33443413

If you know of a relevant reference for GPR52 Comp-43, please let us know.

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Citations for GPR52 Comp-43

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