5.31145

mGlu7 Antagonist, XAP044

• 동의어(들): 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
• 실험식(Hill 표기법): C₁₅H₉IO₄
• CAS Number: 196928-50-4
• Molecular Weight: 380.13
• MDL number: MFCD00525548
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥97% (HPLC)
• Quality Level: 100
• 양식: powder
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: pale yellow
• solubility: DMSO: 100 mg/mL
• 저장 온도: 2-8°C
• SMILES string: Ic1ccc(cc1)Oc2[c](c3c([o]c2)cc(cc3)O)=O
• 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
• InChI key: XXZKJJYWINSUMJ-UHFFFAOYSA-N

설명

일반 설명

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.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
mGlu7R

Reversible: yes

Target IC₅₀: 3.5 and 2.8 &micro

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable