XAP 044

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Cat.No. 5248 - XAP 044 | C15H9IO4 | CAS No. 196928-50-4
Description: Potent and selective mGlu7 antagonist
Chemical Name: 7-Hydroxy-3-(4-iodophenoxy)-4H-1-benzopyran-4-one
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews (1)
Literature

Biological Activity

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.

Technical Data

M. Wt 380.13
Formula C15H9IO4
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 196928-50-4
PubChem ID 5428913
InChI Key XXZKJJYWINSUMJ-UHFFFAOYSA-N
Smiles OC1=CC=C(C(C(OC3=CC=C(I)C=C3)=CO2)=O)C2=C1

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
DMSO 38.01 100
ethanol 7.6 20

Preparing Stock Solutions

The following data is based on the product molecular weight 380.13. 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 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

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References

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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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

Citations for XAP 044

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Reviews for XAP 044

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XAP044 successfully antagonize the effect of L-AP4- stimulated mGlu7 receptors
By Anonymous on 01/05/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: HEK293 cells

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)

PMID: 27769854
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