Biological Activity
Potent, non-competitive excitatory amino acid transporter (EAAT) blocker. Preferentially inhibits glutamate-induced [3H]D-aspartate release (IC50 = 1.2 μM) rather than [3H]L-glutamate uptake (IC50 = 16.9 μM). Moderately selective; displays no affinity for NMDA and metabotropic glutamate receptors, and low affinity for AMPA and kainate receptors (IC50 values are 35 and 45 μM respectively).
Technical Data
M. Wt | 172.14 |
Formula | C6H8N2O4 |
Storage | Store at +4°C |
Purity | ≥98% (HPLC) |
CAS Number | 227619-65-0 |
PubChem ID | 90488748 |
InChI Key | RDIJEATTYWWNKA-ACIRMZHZSA-N |
Smiles | OC1=NO[C@@]2([H])[C@@]([H])1CN[C@@H]2[C@@](O)=O.OC3=NO[C@]4([H])[C@]([H])3CN[C@H]4C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 3.44 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 172.14. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 5.81 mL | 29.05 mL | 58.09 mL |
5 mM | 1.16 mL | 5.81 mL | 11.62 mL |
10 mM | 0.58 mL | 2.9 mL | 5.81 mL |
50 mM | 0.12 mL | 0.58 mL | 1.16 mL |
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References
References are publications that support the products' biological activity.
Conti et al (1999) Synthesis and enantiopharmacology of new AMPA-kainate receptor agonists. J.Med.Chem. 42 4099 PMID: 10514280
Funicello et al (2004) Dissociation of [3H]glutamate uptake from glutamate-induced [3H]D-Aspartate release by 3-hydroxy-4,5,6,6a-tetrahydro-3aH-pyrrolo[3,4-d]isoxazole-4-carboxylic acid and 3-hydroxy-4,5,6,6a-tetrahydro-3aH-pyrro Mol.Pharmacol. 66 522 PMID: 15322243
Conti et al (1999) Synthesis of new bicyclic analogues of glutamic acid. Tetrahedron 55 5623 PMID:
Keywords: (±)-HIP-B, supplier, Potent, non-competitive, EAAT, inhibitors, inhibits, Excitatory, Amino, Acid, Transporters, GLAST, GLT-1, Glutamate, Monoamine, Neurotransmitter, Glutamate, Transporters, Glutamate, Transporters, Tocris Bioscience