ADX-47273

製品コードS2690 バッチS269001

印刷

化学情報

Chemical Structure Synonyms BA 94673139 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C20H17F2N3O2
分子量 369.36 CAS No. 851881-60-2
Solubility (25°C)* 体外 DMSO 74 mg/mL (200.34 mM)
Ethanol 30 mg/mL (81.22 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
30%propylene glycol 5%Tween80 65%D5W
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified propylene glycol stock solution to 50 μL of Tween 80, mix evenly to clarify it; then continue to add 650 μL of D5W to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 ADX47273 (BA 94673139) is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes.
in vitro ADX47273 causes a concentration-dependent increase in the response to 50 nM glutamate in HEK 293 cells expressing rat mGlu5, the maximal increase in the response is approximately 9-fold, with an EC50 of 0.17 ± 0.03 μM. ADX47273 causes a concentration-dependent increase in the response to 300 nM glutamate with an EC50 value of 0.23 ± 0.07 μM in primary astrocyte cultures. ADX47273 at concentration of 0.1 or 1 μM decreases the EC50 for glutamate for 4- and 9-fold, respectively, in HEK 293 cells expressing rat mGlu5. ADX47273 at concentration of 1 or 3 μM decreases the EC50 for glutamate for 4- and 9-fold, respectively, in primary astrocyte cultures. ADX47273 inhibits binding of [3H]MPEP to membranes prepared from HEK 293 cells expressing mGlu5 receptors with Ki of 4.3 ± 0.5 μM. [1] ADX-47273 at concentration of 0.3 μM elicited an enhancement of NMDA-receptor dependent long-term potentiation in rat hippocampal slices, the effect can be blocked in the presence of 10 μM specific mGlu5 receptor antagonist MPEP. [2]
in vivo ADX47273 intraperitoneally administrated at dose of 10 mg/kg increases ERK and CREB phosphorylation in both the prefrontal cortex and hippocampus in Long-Evans rats. ADX47273 intraperitoneally administrated at dose of 10-100 mg/kg produces dose-dependent decreases in avoidance responding and increased escapes at doses that did not produce any response failures in Sprague-Dawley rats. ADX47273 intraperitoneally administrated at dose of 10-300 mg/kg produces a dose-dependent decrease in apomorphine-induced climbing in CF-1 mice. ADX47273 intraperitoneally administrated at dose of 100 mg/kg decreased locomotor activity compared with vehicle pretreatment at 20 min after PCP, 30 min after apomorphine, and at all time points after amphetamine challenge in mice. ADX47273 intraperitoneally administrated at dose of 175 mg/kg lowers dopamine levels in the Sprague-Dawley rat nucleus accumbens. ADX47273 intraperitoneally administrated at dose of 1 to 50 mg/kg increases novel object recognition and reduces impulsivity in the five-choice serial reaction time test in rats. [1] ADX47273 intraperitoneally administrated at dose of 100 mg/kg significantly decreases conditioned avoidance response at 30 and 90 min post-injection in male Sprague-Dawley rats. [3]

プロトコル(参考用のみ)

キナーゼアッセイ Radioligand Binding Assays
[3H]MPEP binding. [3H]MPEP is used to evaluate the interaction of compounds with the receptor. Membranes are prepared from HEK 293 cells expressing rat mGlu5 receptor. Aliquots of these membranes are added to tubes containing ADX47273 (0.4% DMSO final concentration) or vehicle and [3H]MPEP (2 nM final concentration in 50 mM Tris/0.9% NaCl, pH 7.4). The tubes are incubated for 60 min at room temperature with shaking, and the membrane-bound ligand is separated from the free ligand by filtration onto glass fiber filters presoaked with 20 mM HEPES, 2 mM CaCl2, and MgCl2, pH 7.2. Membrane bound radioactivity is determined by scintillation counting of the filters. Competition binding data are analyzed, and Ki is determined using Prism 4.0 . [3H]Quisqualate binding. Membranes from CHO cells expressing rat mGlu5 are resuspended in ice-cold assay buffer (20 mM HEPES-NaOH, pH 7.2, containing 2 mM MgCl2 and 2 mM CaCl2) with 20 nM [3H]quisqualate either in the absence or presence of 10 μM ADX47273 for 1 h at room temperature. Nonspecific binding is defined in the presence of 1 mM glutamate. At the end of the incubation, the suspension is filtered onto Whatman GF/C glass fiber filters and washed rapidly three times with 1 ml of cold binding buffer. The radioactivity trapped on the filters is measured by liquid scintillation in a Tri-Carb model 2500 TR counter.
動物実験 動物モデル male Long-Evans rats
投薬量 10 mg/kg
投与方法 Inject intraperitoneally at a single dose30 min before sacrifice

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Therapeutic molecules and endogenous ligands regulate the interaction between brain cellular prion protein (PrPC) and metabotropic glutamate receptor 5 (mGluR5) [ J Biol Chem, 2014, 289(41):28460-77] PubMed: 25148681

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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