VU 0357121 化学構造
分子量: 305.32

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Quality Control & MSDS

製品説明

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製品の説明

生物活性

製品説明 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。
ターゲット 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
臨床試験
特集

プロトコル (参考用のみ)

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download VU 0357121 SDF
分子量 305.32
化学式

C17H17F2NO2

CAS No. 433967-28-3
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 61 mg/mL (199.79 mM)
エタノール 21 mg/mL (68.78 mM)
<1 mg/mL (<1 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 4-butoxy-N-(2,4-difluorophenyl)benzamide

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description
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