PeptideDB

PEAQX tetrasodium hydrate (NVP-AAM077 tetrasodium hydrate)

PEAQX tetrasodium hydrate (NVP-AAM077 tetrasodium hydrate)

CAS No.:

PEAQX (NVP-AAM077) tetrasodium hydrate is a specific, orally bioavailable NMDA antagonist (inhibitor) with IC50s of 270
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This product is for research use only, not for human use. We do not sell to patients.

PEAQX (NVP-AAM077) tetrasodium hydrate is a specific, orally bioavailable NMDA antagonist (inhibitor) with IC50s of 270 nM and 29600 nM for hNMDAR 1A/2A and hNMDAR 1A/2B, respectively.

Physicochemical Properties


Molecular Formula C17H15BRN3NA4O6P
Molecular Weight 560.15
Related CAS # PEAQX;459836-30-7
Appearance Light yellow to khaki solid powder
HS Tariff Code 2934.99.9001
Storage

Powder-20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


Targets NMDA Receptor
ln Vitro Similar caspase-3 activation is produced by PEAQX (3 μM), although NVP-AAM007 is almost three times more powerful [2].
ln Vivo PEAQX (10–40 mg/kg) enhances cortical caspase-3 activity after subchronic treatment in a dose-dependent manner [2]. In contrast to saline pretreatment, PEAQX (10 and 20 mg/kg) increased locomotor activity in response to PCP challenge (4 mg/kg on PN28–35) [2]. Even with learning and memory impairment, PEAQX (10 mg/kg, i.p.) counteracts the effects of PRE084 on CaMKIV-TORC1-CREB and BDNF [3].
Animal Protocol Animal/Disease Models: Timed, day 14 pregnant female SD (Sprague-Dawley) rats[2].
Doses: 10, 20 or 40 mg/kg.
Route of Administration: SC
Experimental Results: demonstrated a sensitized locomotor response to PCP challenge on PN28-35.

Animal/Disease Models: Timed , day 14 pregnant female SD (Sprague-Dawley) rats[2].
Doses: 4 mg/kg.
Route of Administration: IP
Experimental Results: Did not Dramatically increase locomotor activity in rats treated sub-chronically with PEAQX on PN7, 9 and 11.

Animal/Disease Models: 11 -week old C57BL/6 mice[3].
Doses: 10 mg/kg.
Route of Administration: IP.
Experimental Results: Reversed the effect of PRE084 (F3,78 = 10.446, p<0.01).
References

[1]. 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition. Bioorg Med Chem Lett. 2002 Apr 8;12(7):1099-102.

[2]. Differential role of N-methyl-D-aspartate receptor subunits 2A and 2B in mediating phencyclidine-induced perinatal neuronal apoptosis and behavioral deficits. Neuroscience. 2009 Nov 10;163(4):1181-91.

[3]. Sigma-1 receptor in brain ischemia/reperfusion: Possible role in the NR2A-induced pathway to regulate brain-derived neurotrophic factor. J Neurol Sci. 2017 May 15;376:166-175.


Solubility Data


Solubility (In Vitro) H2O :~25.5 mg/mL (~45.52 mM)
Solubility (In Vivo) Solubility in Formulation 1: 100 mg/mL (178.52 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.7852 mL 8.9262 mL 17.8524 mL
5 mM 0.3570 mL 1.7852 mL 3.5705 mL
10 mM 0.1785 mL 0.8926 mL 1.7852 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.