DL-2-Amino-3-phosphonopropionic acid
An Antagonist of mGluR1 Receptors
Cat #: D-275
Sizes: 50 mg, 100 mg, 250 mg, 500 mg
Source: Synthetic
MW: 169.07 Da.
Target: mGluR1
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DL-AP3 is racemic compound of 2-amino-3-phosphonopropionic acid that acts as a potent and competitive antagonist of mGluR1 receptors. It demonstrates IC50 values of 1 mM for rat mGluR1 when challenged with glutamate2. DL-AP3 has neuroprotective effects in the gerbil model of global ischemia1,2. Glutamate is the most abundant excitatory neurotransmitter in the central nervous system and it modulates activity of many types of synapses by activating in part metabotropic glutamate receptors (mGluRs), members of G-protein coupled receptors (GPCRs). These receptors are divided into three groups based on sequence homology with a total of eight subtypes, mGluR1 to mGluR8. Type 1 mGluRs are mainly detected on post-synaptic neurons and affect the fate of neuronal progenitor cells and neural stem cell, and are important for the formation of the hippocampus3.
Alomone Labs is pleased to offer DL-AP3 (#D-275).
DL-AP3References
Schoepp, D.D. et al. (1999) Neuropharmacology38, 1431.
Hawkinson, J.E. et al. (1996) Eur. J. Pharmacol.307, 219.
Eom, H.S. et al. (2016) PLoS One11, e0147538.
Our Bioassay
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Our bioassay
Alomone Labs DL-AP3 inhibits mGluR1-mediated Ca2+ mobilization in U2OS cells. Dose response of DL-AP3 (#D-275) normalized inhibition of human mGluR1-mediated, L-Glutamate-evoked Ca2+ mobilization. hmGluR1-expressing cells were loaded with calcium-sensitive dye, incubated with a range of DL-AP3 concentrations, and stimulated with 5 µM L-Glutamate (EC80). Changes in intracellular Ca2+ following stimulation were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was determined at 295 µM.
Purity>97%.
Effective concentration0.1-10 mM.
Chemical name2-amino-3-phosphonopropanoic acid.
Molecular formulaC3H8NO5P.
CAS number5652-28-8.
ActivityDL-AP3 is a selective competitive antagonist of group I metabotropic glutamate receptors, at 1 mM suppressing mGluR1 response in an agonist dependent manner1.
Storage before reconstitutionProduct as supplied can be stored at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Reconstitution
Soluble in water, 1eq NaOH and aqueous buffers. Centrifuge all product preparations before use (10000 x g 5 min).