1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. LY404039

LY404039 

Cat. No.: HY-50906 Purity: >98.0%
Handling Instructions

LY404039 is a potent, selective and orally active mGluR2 and mGluR3 agonist with Kis of 149 nM and 92 nM for recombinant human mGluR2 and mGluR3, respectively. LY404039 shows >100-fold selectivity for mGluR2/3 over other receptors/transproters. LY404039 has antipsychotic and anxiolytic effects.

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

LY404039 Chemical Structure

LY404039 Chemical Structure

CAS No. : 635318-11-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 55 In-stock
Estimated Time of Arrival: December 31
5 mg USD 50 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
25 mg USD 200 In-stock
Estimated Time of Arrival: December 31
50 mg USD 350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 610 In-stock
Estimated Time of Arrival: December 31
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Description

LY404039 is a potent, selective and orally active mGluR2 and mGluR3 agonist with Kis of 149 nM and 92 nM for recombinant human mGluR2 and mGluR3, respectively. LY404039 shows >100-fold selectivity for mGluR2/3 over other receptors/transproters. LY404039 has antipsychotic and anxiolytic effects[1].

IC50 & Target[1]

mGlu2 Receptor

149 nM (Ki, Recombinant human mGluR2)

hmGluR3

92 nM (Ki)

In Vitro

LY404039 is a nanomolar potent agonist in rat neurons expressing native mGlu2/3 receptors (Ki = 88 nM)[1].
Functionally, LY404039 potently inhibits Forskolin-stimulated cAMP formation in cells expressing human mGlu2 (EC50 = 23 nM) and mGlu3 receptors (EC50 = 48 nM)[1].
Electrophysiological studies indicate that LY404039 suppresses electrically evoked excitatory activity in the striatum, and serotonin-induced L-glutamate release in the prefrontal cortex. LY404039 suppresses the frequency of 5-HT-induced excitatory postsynaptic currents (EPSCs) with an EC50 of 82.3 nM and with a near maximal suppression of 85.6% at 1 μM[1].
LY404039 inhibits the binding of the D2-specific antagonist, [3H]domperidone, to the human cloned D2 receptor with dissociation constants of 8.2 nM at D2High and 1640 nM at D2Low. Using rat striatal tissue, LY404039 has dissociation constants of 12.6 nM at D2High and 2100 nM at D2Low[2].

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

In Vivo

LY404039 attenuates amphetamine- and phencyclidine-induced hyperlocomotion (3-30 and 10 mg/kg, respectively). LY404039 (3-10 mg/kg) inhibits conditioned avoidance responding. LY404039 also reduces fear-potentiated startle in rats (3-30 μg/kg) and marble burying in mice (3-10 mg/kg), indicating anxiolytic-like effects. LY404039 (10 mg/kg) also increases dopamine and serotonin release/turnover in the prefrontal cortex[3].
Following oral administration of LY404039 to fasted rats at doses of 1, 3, or 10 mg/kg, exposure increased proportionally with dose. LY404039 (10 mg/kg; p.o.) treatment shows the Cmax is 1528.5 ng/mL and Tmax is 2 hours in rats[1].

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

Molecular Weight

235.21

Formula

C₇H₉NO₆S

CAS No.

635318-11-5

SMILES

O=C([[email protected]]1(N)CS([[email protected]@]2([H])[[email protected]](C(O)=O)[[email protected]@]12[H])(=O)=O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

H2O : 5.4 mg/mL (22.96 mM; ultrasonic and adjust pH to 8 with H2O)

DMSO : 3.84 mg/mL (16.33 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.2515 mL 21.2576 mL 42.5152 mL
5 mM 0.8503 mL 4.2515 mL 8.5030 mL
10 mM 0.4252 mL 2.1258 mL 4.2515 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: >98.0%

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Keywords:

LY404039LY 404039LY-404039mGluRMetabotropic glutamate receptorsmGlu2mGlu3antipsychoticanxiolyticcAMPL-glutamateInhibitorinhibitorinhibit

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LY404039
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