211311-95-4
211311-95-4 structure
- Name: LY 404187
- Chemical Name: N-[2-[4-(4-cyanophenyl)phenyl]propyl]propane-2-sulfonamide
- CAS Number: 211311-95-4
- Molecular Formula: C19H22N2O2S
- Molecular Weight: 348.503
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel iGluR
- Create Date: 2016-08-24 09:02:18
- Modify Date: 2024-01-08 15:12:24
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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].
| Name | N-[2-[4-(4-cyanophenyl)phenyl]propyl]propane-2-sulfonamide |
|---|---|
| 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]- |
| 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]. |
|---|---|
| Related Catalog | |
| Target |
EC50: 5.65 µM (GluR1i), 0.15 µM (GluR2i), 1.44 µM (GluR2o), 1.66 µM (GluR3i), 0.21 µM (GluR4i)[2] |
| 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]. |
| 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. |
| References |
| Density | 1.1±0.1 g/cm3 |
|---|---|
| Boiling Point | 498.4±47.0 °C at 760 mmHg |
| Molecular Formula | C19H22N2O2S |
| Molecular Weight | 348.503 |
| Flash Point | 255.2±29.3 °C |
| Exact Mass | 348.187134 |
| PSA | 78.34000 |
| LogP | 4.19 |
| Vapour Pressure | 0.0±1.3 mmHg at 25°C |
| Index of Refraction | 1.546 |
| HS Code | 2935009090 |
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| 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% |