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Submit ReviewGPR52 Comp-43
Description: GPR52 receptor antagonist
Chemical Name: (2E)-5-Phenyl-1-(2-thienyl)-2-penten-1-one
Purity: ≥98% (HPLC)
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.
| 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
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
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Keywords: GPR52 Comp-43, GPR52 Comp-43 supplier, GPR52comp43, receptors, antagonists, antagonism, huntingtons, huntingtin, neuronal, GPCR, CAY10786, GPR52IN43, Orphan, 7-TM, Receptors, 7445, Tocris Bioscience
Citations for GPR52 Comp-43
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