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LY404039

Catalog No. T6022 CAS 635318-11-5

Synonyms: pomaglumetad

LY404039 (pomaglumetad) is an effective agonist of recombinant human mGlu2(Ki =149 nM)/mGlu3(Ki =92 nM).

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LY404039, CAS 635318-11-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 39.00
10 mg	In stock	$ 72.00
25 mg	In stock	$ 163.00
50 mg	In stock	$ 288.00
100 mg	In stock	$ 493.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 99.03%

Purity: 99%

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Description	LY404039 (pomaglumetad) is an effective agonist of recombinant human mGlu2(Ki =149 nM)/mGlu3(Ki =92 nM).
Targets&IC50	mGlu3 (human recombinant):92 nM(Ki), mGlu2 (human recombinant):149 nM(Ki), mGlu2/3 (rat neurons):88 nM(Ki)
In vivo	LY404039 demonstrates higher plasma exposure and better oral bioavailability. LY404039 may be valuable in the treatment of neuropsychiatric disorders, including anxiety and psychosis. [1] In wild-type animals, LY404039 significantly reverses d-amphetamine(AMP)-induced increase in ambulations, distance traveled, and reduced time spent at rest. LY404039 reverses phencyclidine (PCP)-evoked behaviors at 10 mg/kg. The antipsychotic-like effects of LY404039 on PCP and AMP-evoked behavioral activation are absent in mGlu2 and mGlu2/3 but not in mGlu3 receptor-deficient mice. In contrast, clozapine and risperidone inhibit PCP-evoked behaviors in both wild-type and mGlu2/3 receptor-deficient mice. [2] 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 inhibits the expression of alcohol seeking and relapse behavior without altering alcohol self-administration behavior. [3] Moreover, LY404039 attenuates amphetamine- and phencyclidine-induced hyperlocomotion. LY404039 could inhibit conditioned avoidance responding and also reduces fear-potentiated startle in rats and marble burying in mice. Importantly, LY404039 does not produce sedative effects or motor impairment in the conditioned avoidance task. LY404039 also increases dopamine and serotonin release/turnover in the prefrontal cortex. [4]
Kinase Assay	Immunoblotting assay of histone acetylation: PANC-1 cells are treated with 2 μg/mL of Scriptaid for 18 h in culture medium. Treated and untreated cells are harvested with trypsin-EDTA, washed with PBS, and resuspended in a protein sample buffer. Protein concentration is determined by BCA protein assay reagents. Fifty μg of proteins from each sample is loaded on a 12% denaturing polyacrylamide gel. Proteins are subsequently transferred to a nylon membrane using MilliblotGraphite Electroblotter I. The nylon membrane is incubated with rabbit antihuman acetyl-lysine antibody, followed by goat antirabbit antibody coupled to horseradish peroxidase, developed with SuperSignal substrates, and detected by film.

Synonyms	pomaglumetad
Molecular Weight	235.22
Formula	C7H9NO6S
CAS No.	635318-11-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Slightly soluble

References and Literature

1. Rorick-Kehn LM et al. J Pharmacol Exp Ther, 2007, 321(1), 308-317. 2. Fell MJ et al. J Pharmacol Exp Ther, 2008, 326(1), 209-217. 3. Rodd ZA et al. Behav Brain Res, 2006, 171(2), 207-215. 4. Rorick-Kehn LM et al. Psychopharmacology (Berl), 2007, 193(1), 121-136.

Related compound libraries

This product is contained In the following compound libraries：

Nuclear Receptor Compound Library Endocrinology-Hormone Compound Library Anti-Cancer Compound Library Neuronal Signaling Compound Library NO PAINS Compound Library Bioactive Compound Library Glutamine Metabolism Compound Library Bioactive Compounds Library Max Neurotransmitter Receptor Compound Library ReFRAME Related Library

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Keywords

LY404039 635318-11-5 Endocrinology/Hormones Neuroscience GluR Glucocorticoid Receptor inhibit Metabotropic glutamate receptors mGluR cAMP LY-404039 pomaglumetad mGlu3 L-glutamate mGlu2 Inhibitor LY 404039 anxiolytic antipsychotic inhibitor

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