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Description: Selective positive allosteric modulator of AMPA receptors
Chemical Name: N-[2-(4'-Cyano[1,1'-biphenyl]-4-yl)propyl]-2-propanesulfonamide
Purity: ≥98% (HPLC)
Biological Activity for LY 404187
LY 404187 is a selective AMPA receptor positive allosteric modulator (IC50 values are 0.15, 0.21, 1.66 and 5.65 μM for GluA2i, GluA4i, GluA3i and GluA1i respectively). Potentiates glutamate and AMPA-evoked currents in prefrontal cortex (PFC) pyramidal neurons in vitro. Has no effect on NMDA- or kainate-evoked currents; also has no effect on K+ or Na+ ion channels. Potentiates PFC glutamatergic synaptic transmission in vitro and in vivo. Induces neurite growth in combination with (S)-AMPA (Cat. No. 0254) in SH-SY5Y human neuroblastoma cells in vitro. Also reduces MPTP-induced toxicity in mice. Brain penetrant.
Compound Libraries for LY 404187
LY 404187 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for LY 404187
| M. Wt | 342.46 |
| Formula | C19H22N2O2S |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 211311-95-4 |
| PubChem ID | 9928016 |
| InChI Key | HOQAVGZLYRYHSO-UHFFFAOYSA-N |
| Smiles | N#CC1=CC=C(C2=CC=C(C(C)CNS(C(C)C)(=O)=O)C=C2)C=C1 |
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 LY 404187
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.25 | 100 | |
| ethanol | 17.12 | 50 |
Preparing Stock Solutions for LY 404187
The following data is based on the product molecular weight 342.46. 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 | 2.92 mL | 14.6 mL | 29.2 mL |
| 5 mM | 0.58 mL | 2.92 mL | 5.84 mL |
| 10 mM | 0.29 mL | 1.46 mL | 2.92 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.58 mL |
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Product Datasheets for LY 404187
References for LY 404187
References are publications that support the biological activity of the product.
O'Neill et al (2004) Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson's disease. Eur.J.Pharmacol. 486 163 PMID: 14975705
Quirk and Nisenbaum (2002) LY404187: a novel positive allosteric modulator of AMPA receptors. CNS Drug Rev. 8 255 PMID: 12353058
Voss et al (2007) Molecular mechanisms of neurite growth with AMPA receptor potentiation. Neuropharmacology 52 590 PMID: 17101156
Baumbarger et al (2001) Positive modulation of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors in prefrontal cortical pyramidal neurons by a novel allosteric potentiator. J.Pharmacol.Exp.Ther. 298 86 PMID: 11408529
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Keywords: LY 404187, LY 404187 supplier, LY404187, selective, ampa, receptors, positive, allosteric, modulators, PAMs, GLUA1, GLUA2, GLUA3, GLUA4, GLUR1, GLUR2, GLUR3, GLUR4, parkinson, disease, depression, memory, AMPA, Receptors, 5297, Tocris Bioscience
Citations for LY 404187
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Literature in this Area
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