1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR
  3. LY-404187

LY-404187 

Cat. No.: HY-13456
Handling Instructions

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.

For research use only. We do not sell to patients.

LY-404187 Chemical Structure

LY-404187 Chemical Structure

CAS No. : 211311-95-4

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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].

IC50 & 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].

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].

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.
Molecular Weight

342.46

Formula

C19H22N2O2S

CAS No.
SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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LY-404187
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HY-13456
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