5.31145

mGlu7 Antagonist, XAP044

• Sinónimos: mGlu7 Antagonist, XAP044, 7-Hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one, 7-Hydroxy-3-(4-iodophenoxy)-chromen-4-one, Metabotropic Glutamate Receptor Subtype 7 Antagonist, XAP-044
• Fórmula empírica (notación de Hill): C₁₅H₉IO₄
• Número de CAS: 196928-50-4
• Peso molecular: 380.13
• Número MDL: MFCD00525548
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Análisis: ≥97% (HPLC)
• Nivel de calidad: 100
• formulario: powder
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: pale yellow
• solubilidad: DMSO: 100 mg/mL
• temp. de almacenamiento: 2-8°C
• InChI: 1S/C15H9IO4/c16-9-1-4-11(5-2-9)20-14-8-19-13-7-10(17)3-6-12(13)15(14)18/h1-8,17H
• Clave InChI: XXZKJJYWINSUMJ-UHFFFAOYSA-N

Descripción

Descripción general

A blood-brain barrier permeable and bioavailable chromenone compound that acts as a potent, selective, and reversible antagonist of mGlu7 receptor (IC₅₀ = 3.5 and 2.8 µM for mGlu7a and mGlu7b in CHO cells). Docks within the Venus flytrap domain (VFTD) close to the binding site of L-glutamate and functions as an orthosteric-like antagonist. Reduces DL-2-amino-4-phosphonobutyric acid (DL-AP4)-induced activation of human mGlu7b receptor (IC₅₀ = 2.8 µM), but does not affect DL-AP4-induced activation of [³⁵S]GTPγS binding by mGlu4 and mGlu6. Shown to diminish [³⁵S]GTPγS binding by the human mGlu7/6 chimeric receptor harboring mGlu7 VFTD (IC₅₀ = 2.5 µM). Displays weak binding affinity towards mGlu5 and mGlu8 receptors (IC₅₀ >20 and 33 µM, respectively) and has no effect on GABA-induced activation of [³⁵S]GTPγS binding by GABA-B receptors. Displays antidepressant and anxiolytic-like properties and selectively blocks long-term potentiation (LTP) in the lateral amygdala of wild type (IC₅₀ = 88 nM), but not of mGlu7- deficient mice.

A blood-brain barrier permeable and bioavailable chromenone compound that acts as a potent, selective, and reversible antagonist of mGlu7 receptor (IC₅₀ = 3.5 and 2.8 µM for mGlu7a and mGlu7b in CHO cells). Docks within the Venus flytrap domain (VFTD) close to the binding site of L-glutamate and functions as an orthosteric-like antagonist. Reduces DL-2-amino-4-phosphonobutyric acid (DL-AP4)-induced activation of human mGlu7b receptor (IC₅₀ = 2.8 µM), but does not affect DL-AP4-induced activation of [³⁵S]GTPγS binding by mGlu4 and mGlu6. Shown to diminish [³⁵S]GTPγS binding by the human mGlu7/6 chimeric receptor harboring mGlu7 VFTD (IC₅₀ = 2.5 µM). Displays weak binding affinity towards mGlu5 and mGlu8 receptors (IC₅₀ >20 and 33 µM, respectively) and has no effect on GABA-induced activation of [³⁵S]GTPγS binding by GABA-B receptors. Displays antidepressant and anxiolytic-like properties and selectively blocks long-term potentiation (LTP) in the lateral amygdala of wild type (IC₅₀ = 88 nM), but not of mGlu7- deficient mice.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

Acciones bioquímicas o fisiológicas

Cell permeable: yes

Primary Target
mGlu7R

Reversible: yes

Target IC₅₀: 3.5 and 2.8 &micro

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Otras notas

Gee, C.E., et al. 2014. J. Biol. Chem.289, 10975.

Información legal

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable