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LY404039

Cat. No. M1926
LY404039 Structure
Size Price Availability Quantity
5mg USD 50  USD50 In stock
10mg USD 90  USD90 In stock
50mg USD 330  USD330 In stock
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Quality Control & Documentation
Biological Activity

LY404039 is a selective agonist for the metabotropic glutamate receptor (mGluR)2/3 receptors. mGluR2 acts as a glutamatergic autoreceptor in the brain regions that are believed to be important in the pathophysiology of schizophrenia, such as the prefrontal cortex, striatum, hippocampal formation and the thalamus. LY404039 potently inhibits forskolin-stimulated cAMP formation in cells expressing human mGlu2 and mGlu3 receptors. LY404039 reduces responding on the EtOH in the pavlovian spontaneous recovery (PSR) test and reduces the expression of an alcohol deprivation effect (ADE) during relapse, but does not affect EtOH responding under maintenance conditions. LY404039 also increases dopamine and serotonin release/turnover in the prefrontal cortex.

Customer Product Validations & Biological Datas
Source Pharmacol Res Perspect (2015). Figure 2. LY404039
Method s.c.
Cell Lines Mice
Concentrations 0.63, 2.5, 10 mg/kg
Incubation Time 0.5 h
Results JNJ-40411813, JNJ-42153605, and LY404039 dose dependently inhibited spontaneous locomotion and PCP- and scopolamine-induced hyperlocomotion but not damphetamine- induced hyperlocomotion
Protocol (for reference only)
Cell Experiment
Cell lines RGT cells expressing human mGlu receptors
Preparation method For cAMP assays, cells expressing human mGlu2, mGlu3, mGlu4, mGlu6, mGlu7, or mGlu8 were washed (two times with 200 μl/well) with assay medium (Dulbecco's phosphate-buffered saline plus 3 mM glucose and 500 μM isobutymethylxanthine). The media were replaced with 0.2 ml/well of the same solution, and cells were preincubated for 30 min at 37°C under 95% O2, 5%CO2. Each well was then washed two successive times with 200 μl of medium. Compounds of interest or water vehicle were added, along with forskolin solution (15 μM final concentration group II mGlu receptors, 1 μM final concentration group III mGlu receptors, and total incubation volume 0.1 ml), and cells were further incubated at 37°C under 95% O2, 5%CO2 for 20 min. The incubation was terminated by adding 0.1 ml of 0.2% Triton X-100 lysing solution. Levels of cAMP were determined by a cAMP-125I Scintillation Proximity Assay Screening Biotrak Assay kit (GE Healthcare).
Concentrations 0~10mM
Incubation time 20 min
Animal Experiment
Animal models PCP-Induced mouse model
Formulation 0.9% saline
Dosages 10 mg/kg
Administration i.p.
Chemical Information
Molecular Weight 235.21
Formula C7H9NO6S
CAS Number 635318-11-5
Solubility (25°C) DMSO 1 mg/mL (Need ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Fell MJ, et al. J Pharmacol Exp Ther. Evidence for the role of metabotropic glutamate (mGlu)2 not mGlu3 receptors in the preclinical antipsychotic pharmacology of the mGlu2/3 receptor agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]hexane-4,6-dicarboxylic acid (LY404039).

[2] Rorick-Kehn LM, et al. Psychopharmacology (Berl). In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonist LY404039 in animal models of psychiatric disorders.

[3] Rorick-Kehn LM, et al. J Pharmacol Exp Ther. Pharmacological and pharmacokinetic properties of a structurally novel, potent, and selective metabotropic glutamate 2/3 receptor agonist: in vitro characterization of agonist (-)-(1R,4S,5S,6S)-4-amino-2-sulfonylbicyclo[3.1.0]-hexane-4,6-dicarboxylic acid (LY404039).

[4] Rodd ZA, et al. Behav Brain Res. The metabotropic glutamate 2/3 receptor agonist LY404039 reduces alcohol-seeking but not alcohol self-administration in alcohol-preferring (P) rats.

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