LY-404187
Based on 1 Customer Validation
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.
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- Pureté: 98.27%
- CAS No.: 211311-95-4
- Formule: C19H22N2O2S
- Masse moléculaire:342.46
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Membrane Receptor-targeted Compound Library
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Ion Channel Compound Library
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Allosteric Modulators (AMs) Compound Library
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Activité biologique
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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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.29 μM
Compound: 20
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Inhibition of GluR4 expressed in HEK293 cells
Inhibition of GluR4 expressed in HEK293 cells
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[PMID: 20839777] |
| HEK293 | EC50 |
0.29 μM
Compound: 22g
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Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells
Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells
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[PMID: 11087558] |
| HEK293 | EC50 |
1.44 μM
Compound: 20
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Inhibition of GluR2 flop expressed in HEK cells
Inhibition of GluR2 flop expressed in HEK cells
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[PMID: 20839777] |
| HEK293 | EC50 |
1.66 μM
Compound: 20
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Inhibition of GluR3 expressed in HEK cells
Inhibition of GluR3 expressed in HEK cells
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[PMID: 20839777] |
| HEK293 | EC50 |
1061 nM
Compound: 5b
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Activity against human GLUR4 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
Activity against human GLUR4 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
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[PMID: 16879964] |
| HEK293 | EC50 |
1905 nM
Compound: 5b
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Activity against human GLUR2 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
Activity against human GLUR2 flop expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
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[PMID: 16879964] |
| HEK293 | EC50 |
290 nM
Compound: 3a
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Potentiation of responses mediated by 100 uM L-glutamate in transfected HEK293 cells expressing human homomeric iGluR4 flip receptors.
Potentiation of responses mediated by 100 uM L-glutamate in transfected HEK293 cells expressing human homomeric iGluR4 flip receptors.
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[PMID: 11985477] |
| HEK293 | EC50 |
420 nM
Compound: 5b
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Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
Activity against human GLUR4 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
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[PMID: 16879964] |
| HEK293 | EC50 |
5.65 μM
Compound: 20
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Inhibition of GluR1 expressed in HEK cells
Inhibition of GluR1 expressed in HEK cells
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[PMID: 20839777] |
| HEK293 | EC50 |
559 nM
Compound: 5b
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Activity against human GLUR2 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
Activity against human GLUR2 flip expressed in HEK293 cells assessed as glutamate-stimulated calcium influx by FLIPR assay
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[PMID: 16879964] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (20-25 g) are challenged with MPTP on day 8[4]
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Dosage:0.5 mg/kg
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Administration:S.c; twice daily on weekdays and once daily at weekends for 11 days
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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.
Chemical Information
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CAS No. 211311-95-4
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Appearance Solid
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Masse moléculaire 342.46
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Formule C19H22N2O2S
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Color White to off-white
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SMILES
CC(S(=O)(NCC(C1=CC=C(C2=CC=C(C#N)C=C2)C=C1)C)=O)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (292.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Quirk JC, et, al. LY404187: a novel positive allosteric modulator of AMPA receptors. CNS Drug Rev. Fall 2002; 8(3): 255-82. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9200 mL | 14.6002 mL | 29.2005 mL | 73.0012 mL |
| 5 mM | 0.5840 mL | 2.9200 mL | 5.8401 mL | 14.6002 mL | |
| 10 mM | 0.2920 mL | 1.4600 mL | 2.9200 mL | 7.3001 mL | |
| 15 mM | 0.1947 mL | 0.9733 mL | 1.9467 mL | 4.8667 mL | |
| 20 mM | 0.1460 mL | 0.7300 mL | 1.4600 mL | 3.6501 mL | |
| 25 mM | 0.1168 mL | 0.5840 mL | 1.1680 mL | 2.9200 mL | |
| 30 mM | 0.0973 mL | 0.4867 mL | 0.9733 mL | 2.4334 mL | |
| 40 mM | 0.0730 mL | 0.3650 mL | 0.7300 mL | 1.8250 mL | |
| 50 mM | 0.0584 mL | 0.2920 mL | 0.5840 mL | 1.4600 mL | |
| 60 mM | 0.0487 mL | 0.2433 mL | 0.4867 mL | 1.2167 mL | |
| 80 mM | 0.0365 mL | 0.1825 mL | 0.3650 mL | 0.9125 mL | |
| 100 mM | 0.0292 mL | 0.1460 mL | 0.2920 mL | 0.7300 mL |
LY-404187 Related Classifications
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