Pomaglumetad (LY404039)

Alias: LY-404039; LY 404039; Pomaglumetad;LY404039; LY-404,039; LY404,039; LY 404,039
Cat No.:V1079 Purity: ≥98%
Pomaglumetad (LY404039; LY-404039; LY-404,039; LY404,039) is a novel and potent agonist of recombinant human mGlu2/mGlu3 receptors with the potential for the treatment of Schizophrenia.
Pomaglumetad (LY404039) Chemical Structure CAS No.: 635318-11-5
Product category: GluR
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Pomaglumetad (LY404039; LY-404039; LY-404,039; LY404,039) is a novel and potent agonist of recombinant human mGlu2/mGlu3 receptors with the potential for the treatment of Schizophrenia. It activates mGlu2/mGlu3 receptors with Ki values of 149 nM/92 nM, and exhibits >100-fold selectivity for mGlu2/mGlu3 over ionotropic glutamate receptors, glutamate transporters, and other receptors. The inhibition of forskolin-stimulated cAMP formation has indicated that LY404039 was a nanomolar potent agonist of human mGlu2 (EC50 = 23 nM) and mGlu3 (EC50 = 48 nM) receptors.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
In rats with neurons expressing native mGlu2/3 receptors (Ki=88 nM), LY404039 is a nanomolar potent agonist [1]. Functioning as a potent inhibitor of forskolin-stimulated cAMP formation, LY404039 acts on cells that express human mGlu2 (EC50=23 nM) and mGlu3 (EC50=48 nM) receptors [1]. According to electrophysiological research, LY404039 suppresses serotonin-induced L-glutamate release in the prefrontal cortex and electrically evoked excitatory activity in the striatum. LY404039 exhibits a maximum inhibition of 85.6% at 1 μM, effectively suppressing the frequency of 5-HT-induced excitatory postsynaptic currents (EPSC) with an EC50 of 82.3 nM [1]. LY404039 blocks the human cloned D2 receptor from binding to the D2-specific antagonist [3H]domperidone, with a dissociation constant of 8.2 nM for high D2 and 1640 nM for low D2. The dissociation constants of LY404039 were determined using rat striatal tissue, and they were 12.6 nM at D2 high and 2100 nM at D2 low [2].
ln Vivo
LY404039 reduces hyperkinesis brought on by amphetamines (3–30 mg/kg) and phencyclidines (10 mg/kg), respectively. The conditioned avoidance responses are inhibited by LY404039 (3–10 mg/kg). Additionally, marble burying in mice (3–10 mg/kg) and fear-potentiated startle in rats (3–30 μg/kg) are both decreased by LY404039, indicating anxiolytic-like effects. Additionally, LY404039 (10 mg/kg) enhances serotonin and dopamine release/turnover in the prefrontal cortex [3]. Exposure increased proportionately with the dose after LY404039 was given orally to fasting rats at doses of 1, 3, or 10 mg/kg. In rats treated with LY404039 (10 mg/kg; po), the Cmax was 1528.5 ng/mL and the Tmax was 2 hours [1].
Animal Protocol
Dissolved in 0.9% saline and the pH is adjusted to 6.0 with 1 M NaOH; 10 mg/kg; i.p. injection
Separate mGlu2 and mGlu3 receptor knockout mice are established
References
[1]. Linda M Rorick-Kehn, et al. 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). J Pharmacol Exp Ther. 2007 Apr;321(1):308-17.
[2]. Seeman P. An agonist at glutamate and dopamine D2 receptors, LY404039. Neuropharmacology. 2013 Mar;66:87-8.
[3]. Rorick-Kehn LM, et al. In vivo pharmacological characterization of the structurally novel, potent, selective mGlu2/3 receptor agonistLY404039 in animal models of psychiatric disorders. Psychopharmacology (Berl). 2007 Jul;193(1):121-36.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C7H9NO6S
Molecular Weight
235.22
CAS #
635318-11-5
SMILES
O=C([C@]1(N)CS([C@@]2([H])[C@H](C(O)=O)[C@@]12[H])(=O)=O)O
Synonyms
LY-404039; LY 404039; Pomaglumetad;LY404039; LY-404,039; LY404,039; LY 404,039
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 1 mg/mL (4.3 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.2513 mL 21.2567 mL 42.5134 mL
5 mM 0.8503 mL 4.2513 mL 8.5027 mL
10 mM 0.4251 mL 2.1257 mL 4.2513 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Biological Data
  • LY404039

    Displacement of [3H]LY341495 binding to mGlu receptors by LY354740 or LY404039 in forebrain tissue from adult rats (200–500 μg) or RGT cells expressing the designated receptors.J Pharmacol Exp Ther.2008 Jul;326(1):209-17.
  • LY404039

    Selective inhibition of forskolin-stimulated cAMP formation by LY354740 or LY404039 in cells expressing group II (mGlu2 and mGlu3), but not group III (mGlu4, -6, -7, and -8) receptors.J Pharmacol Exp Ther.2008 Jul;326(1):209-17.
  • LY404039

    Effects of LY404039 on EPSPs evoked in striatal neurons in vitro.J Pharmacol Exp Ther.2008 Jul;326(1):209-17.
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