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

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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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 110 In-stock
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10 mg USD 170 In-stock
25 mg USD 340 In-stock
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Based on 1 publication(s) in Google Scholar

LY-404187 Related Antibodies

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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].

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

LY-404187 Related Antibodies
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.
Molecular Weight

342.46

Formula

C19H22N2O2S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9200 mL 14.6002 mL 29.2005 mL
5 mM 0.5840 mL 2.9200 mL 5.8401 mL
View the 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.

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Purity & Documentation
References

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
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LY-404187 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LY-404187211311-95-4LY404187LY 404187iGluRIonotropic glutamate receptorsAllostericAMPAGluR1iGluR2iGluR2oGluR3iGluR4ipsychiatricneurodegenerativeInhibitorinhibitorinhibit

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