5.31145

mGlu7 Antagonist, XAP044

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₁₅H₉IO₄
• Numer CAS: 196928-50-4
• Masa cząsteczkowa: 380.13
• Numer MDL: MFCD00525548
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Próba: ≥97% (HPLC)
• Poziom jakości: 100
• Postać: powder
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: pale yellow
• rozpuszczalność: DMSO: 100 mg/mL
• temp. przechowywania: 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
• Klucz InChI: XXZKJJYWINSUMJ-UHFFFAOYSA-N

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
mGlu7R

Reversible: yes

Target IC₅₀: 3.5 and 2.8 &micro

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Rekonstytucja

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

Inne uwagi

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

Informacje prawne

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

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable