VU 0357121 化学構造
分子量: 305.32


Quality Control & MSDS


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情報 VU 0357121は、33nMのEC50によるmGlu5レセプターの新しいアロステリックモジュレーターです。
目標 mGlu5
IC50 33 nM [1]
In vitro試験 VU0357121 do not bind at the MPEP allosteric site of mGlu5, thus do not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU0357121 to shift the glutamate concentration−response curve, whereas the response to VU0357121 is not altered by the F585I/rmGlu5 mutation. [1] VU0357121 show weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line. [2]
In vivo試験

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ: [1]

Radioligand Binding Assay The allosteric antagonist MPEP analogue [3H]methoxyPEPy is used to evaluate the ability of test compounds to interact with the MPEP site on mGlu5. Membranes are prepared from rat mGlu5 HEK293 cells. VU0357121 is diluted in assay buffer (50 mM Tris/0.9% NaCl, pH 7.4) to a 5× stock, and 100 μL of the test compound is added to each well of a 96 deep-well assay plate. Three hundred microliter aliquots of membranes diluted in assay buffer (20 μg/well) are added to each well. One hundred microliters of [3H]methoxyPEPy (2 nM final concentration) is added, and the reaction is incubated at room temperature for 1 h with shaking. After the incubation period, the membrane-bound ligand is separated from free ligand by filtration through glass-fiber 96-well filter plates. The contents of each well are transferred simultaneously to the filter plate and washed 3−4 times with assay buffer using a cell harvester. Forty microliters of scintillation fluid is added to each well and the membrane-bound radioactivity determine by scintillation counting. Nonspecific binding is estimated using 5 μM MPEP. Concentration−response curves are generated using a four parameter logistical equation in GraphPad Prism.



Download VU 0357121 SDF
分子量 305.32


CAS No. 433967-28-3
別名 N/A
溶解度 (25°C)
  • DMSO 61 mg/mL
  • 水 <1 mg/mL
  • エタノール 21 mg/mL
保管 2年 -20°C
6月-80°Cin DMSO
化学名 4-butoxy-N-(2,4-difluorophenyl)benzamide




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