Introduction：Basic information about CAS 211311-95-4|LY 404187, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | LY 404187 |
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| CAS Number | 211311-95-4 | Molecular Weight | 348.503 |
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| Density | 1.1±0.1 g/cm3 | Boiling Point | 498.4±47.0 °C at 760 mmHg |
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| Molecular Formula | C19H22N2O2S | Melting Point | / |
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| MSDS | / | Flash Point | 255.2±29.3 °C |
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Names
| Name | N-[2-[4-(4-cyanophenyl)phenyl]propyl]propane-2-sulfonamide |
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| Synonym | More Synonyms |
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LY 404187 BiologicalActivity
| Description | LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases[1][2]. |
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| Related Catalog | Signaling Pathways >>Neuronal Signaling >>iGluRResearch Areas >>Neurological DiseaseSignaling Pathways >>Membrane Transporter/Ion Channel >>iGluR |
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| Target | EC50: 5.65 µM (GluR1i), 0.15 µM (GluR2i), 1.44 µM (GluR2o), 1.66 µM (GluR3i), 0.21 µM (GluR4i)[2] |
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| In Vitro | LY-404187 (3-10 nM) potentiates glutamate-evoked inward currents in human GluR4 transfected HEK293 cells[2]. LY-404187 (0.03-10 µM) selectively enhances glutamate-evoked currents through AMPA receptor/channels of acutely isolated pyramidal neurons with considerably greater potency (EC50=1.3±0.3 µM) and efficacy (Emax=45.3±8.0-fold increase) [3]. LY-404187 does not affect the magnitude or time course of wholecell K+ or Na+ currents in pre frontal cortex (PFC) pyramidal neurons at concentrations of 10 µM[3]. |
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| In Vivo | LY-404187 (0.5 mg/kg; s.c for 11 days) can prevents MPTP-induced neurotoxicity in mice[4]. LY-404187 (0.5 mg/kg; s.c. for 28 days) attenuates apomorphine-induced contraversive rotations and affords significant protection against the loss of tyrosine hydroxylase positive nigral cell bodies[4]. LY-404187 (0.1 or 0.5 mg/kg; s.c. for 14 days) affords functional, neurochemical and histological protection after infusion of 6-hydroxydopamine into the substantia nigra in rats[4]. LY-404187 (0.5 mg/kg; s.c. for 14 days) delayed treatment provides functional and histological improvement, suggesting a trophic action as administration is initiated after cell death[4]. LY-404187 (0.1 and 0.5 mg/kg; s.c. for 14 days) increases GAP-43 immunoreactivity in the striatum in a dose-dependent manner[4]. Animal Model: Male C57BL/6J mice (20-25 g) are challenged with MPTP on day 8[4] Dosage: 0.5 mg/kg Administration: S.c; twice daily on weekdays and once daily at weekends for 11 days Result: Attenuated the loss of tyrosine hydroxylase immunoreactivity in the substantia nigra. No significant change in tyrosine hydroxylase immunoreactivity in the dorsal and ventral striatum. |
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| References | [1]. Quirk JC, et, al. LY404187: a novel positive allosteric modulator of AMPA receptors. CNS Drug Rev. Fall 2002; 8(3): 255-82. [2]. Miu P, et, al. Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. Neuropharmacology. 2001 Jun; 40(8): 976-83. [3]. Baumbarger PJ, et, al. 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. 2001 Jul; 298(1): 86-102. [4]. O'Neill MJ, et, al. Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson's disease. Eur J Pharmacol. 2004 Feb 20; 486(2): 163-74. |
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Chemical & Physical Properties
| Density | 1.1±0.1 g/cm3 |
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| Boiling Point | 498.4±47.0 °C at 760 mmHg |
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| Molecular Formula | C19H22N2O2S |
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| Molecular Weight | 348.503 |
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| Flash Point | 255.2±29.3 °C |
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| Exact Mass | 348.187134 |
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| PSA | 78.34000 |
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| LogP | 4.19 |
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| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
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| Index of Refraction | 1.546 |
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| InChIKey | HOQAVGZLYRYHSO-UHFFFAOYSA-N |
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| SMILES | CC(CNS(=O)(=O)C(C)C)c1ccc(-c2ccc(C#N)cc2)cc1 |
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Safety Information
Customs
| HS Code | 2935009090 |
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| Summary | 2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0% |
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Synonyms
| N-[2-(4'-Cyano[1,1'-biphenyl]-4-yl)propyl]-2-propanesulfonamide |
| N-(2-(4'-Cyano-[1,1'-biphenyl]-4-yl)propyl)propane-2-sulfonamide |
| LY-404,187 |
| N-(2-(4'-cyanobiphenyl-4-yl)propyl)propane-2-sulfonamide |
| QCR-19 |
| N-{2-[4-(4-Cyanophenyl)cyclohexyl]propyl}-2-propanesulfonamide |
| 2-Propanesulfonamide, N-[2-[4-(4-cyanophenyl)cyclohexyl]propyl]- |
