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XAP 044 is a potent and selective mGlu7 antagonist (IC50 = 88 nM); inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice. Displays no effects on the LTP of mGlu7 deficient mice. Exhibits novel activity by binding to the mGlu7 Venus flytrap domain (VFTD). Exhibits anti-anxiety effects in rodent models. Brain penetrant.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
The following data is based on the product molecular weight 380.13. Batch specific molecular weights may vary from batch to batch due to the degree 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||2.63 mL||13.15 mL||26.31 mL|
|5 mM||0.53 mL||2.63 mL||5.26 mL|
|10 mM||0.26 mL||1.32 mL||2.63 mL|
|50 mM||0.05 mL||0.26 mL||0.53 mL|
References are publications that support the biological activity of the product.
Gee et al (2014) Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior. J.Biol.Chem. 289 10975 PMID: 24596089
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View all Glutamate (Metabotropic) Group III Receptor Antagonists
Keywords: XAP 044, XAP 044 supplier, XAP044, potent, specific, mGlu7, antagonists, glutamate, metabotropic, group, III, receptors, venus, flytrap, domain, VFTD, anti-anxiety, Brain, penetrant, Glutamate, (Metabotropic), Group, Receptors, 5248, Tocris Bioscience
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We have studied the cross-talk between mGlu7 and alpha1-adrenergic receptor in recombinant HEK293 cells and XAP 044 was successfully used to antagonize the effect of L-AP4. Briefly, after transfection, we measured the modulation of L-AP4, the mGlu7 receptor agonist on phenylephrine-induced stimulation of inositol phosphates formation. The effect of L-AP4 was antagonised by XAP044 (at 10 and 100 micromolar)
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