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

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
1 mg USD 25 In-stock
5 mg USD 50 In-stock
10 mg USD 90 In-stock
25 mg USD 200 In-stock
50 mg USD 350 In-stock
100 mg USD 560 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

MedChemExpress (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].

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

Molecular Weight

235.21

Formula

C7H9NO6S

CAS No.
Appearance

Solid

Color

White to gray

SMILES

O=C([C@]1(N)CS([C@@]2([H])[C@H](C(O)=O)[C@@]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 : 5.2 mg/mL (22.11 mM; ultrasonic and adjust pH to 6 with NaOH)

DMSO : 3.84 mg/mL (16.33 mM; Need ultrasonic and warming; 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 4.2515 mL 21.2576 mL 42.5152 mL
5 mM 0.8503 mL 4.2515 mL 8.5030 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 2 mg/mL (8.50 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: ≥98.0%

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 / H2O 1 mM 4.2515 mL 21.2576 mL 42.5152 mL 106.2880 mL
5 mM 0.8503 mL 4.2515 mL 8.5030 mL 21.2576 mL
10 mM 0.4252 mL 2.1258 mL 4.2515 mL 10.6288 mL
15 mM 0.2834 mL 1.4172 mL 2.8343 mL 7.0859 mL
H2O 20 mM 0.2126 mL 1.0629 mL 2.1258 mL 5.3144 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

LY404039 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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
LY404039
Cat. No.:
HY-50906
Quantity:
MCE Japan Authorized Agent: