Art. -Nr.: HY-13456

LY-404187

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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.

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Reinheit: 98.27%
CAS. Nr.: 211311-95-4
Formel: C₁₉H₂₂N₂O₂S
Molecular Weight:342.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

LY-404187 Chemical Structure

CAS. Nr.: 211311-95-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EC50: 5.65 µM (GluR1i), 0.15 µM (GluR2i), 1.44 µM (GluR2o), 1.66 µM (GluR3i), 0.21 µM (GluR4i)^[2]

Alle iGluR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	0.29 μM Compound: 20	Inhibition of GluR4 expressed in HEK293 cells Inhibition of GluR4 expressed in HEK293 cells	[PMID: 20839777]
HEK293	EC₅₀	0.29 μM Compound: 22g	Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells Tested for potentiation towards human iGluR4 receptor expressed in HEK293 cells	[PMID: 11087558]
HEK293	EC₅₀	1.44 μM Compound: 20	Inhibition of GluR2 flop expressed in HEK cells Inhibition of GluR2 flop expressed in HEK cells	[PMID: 20839777]
HEK293	EC₅₀	1.66 μM Compound: 20	Inhibition of GluR3 expressed in HEK cells Inhibition of GluR3 expressed in HEK cells	[PMID: 20839777]
HEK293	EC₅₀	1061 nM Compound: 5b	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	[PMID: 16879964]
HEK293	EC₅₀	1905 nM Compound: 5b	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	[PMID: 16879964]
HEK293	EC₅₀	290 nM Compound: 3a	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.	[PMID: 11985477]
HEK293	EC₅₀	420 nM Compound: 5b	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	[PMID: 16879964]
HEK293	EC₅₀	5.65 μM Compound: 20	Inhibition of GluR1 expressed in HEK cells Inhibition of GluR1 expressed in HEK cells	[PMID: 20839777]
HEK293	EC₅₀	559 nM Compound: 5b	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	[PMID: 16879964]

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 (E_max=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.

In Vivo

LY-404187 (0.5 mg/kg; s.c for 11 days) can prevent 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Chemical Information

CAS. Nr. 211311-95-4
Appearance Solid
Molecular Weight 342.46
Formel C₁₉H₂₂N₂O₂S
Color White to off-white
SMILES

CC(S(=O)(NCC(C1=CC=C(C2=CC=C(C#N)C=C2)C=C1)C)=O)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9200 mL

14.6002 mL

29.2005 mL

5 mM

0.5840 mL

2.9200 mL

5.8401 mL

10 mM

0.2920 mL

1.4600 mL

2.9200 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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LY-404187

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Neurotransmitter Receptor Compound Library

Neurodegenerative Disease-related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Allosteric Modulators (AMs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle iGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LY-404187

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

CNS-Penetrant Compound Library

Neurotransmitter Receptor Compound Library

Neurodegenerative Disease-related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Ion Channel Compound Library

Allosteric Modulators (AMs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Alle iGluR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LY-404187 Related Classifications

HY-13456 Related Classifications