| CAS NO: | 851881-60-2 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 200mg | 电议 |
| Cas No. | 851881-60-2 |
| 别名 | (S)-(4-氟苯基)-{3-[3-(4-氟苯基)-[1,2,4]二唑-5-基]哌啶-1-基}甲酮 |
| 化学名 | (4-fluorophenyl)-[(3S)-3-[3-(4-fluorophenyl)-1,2,4-oxadiazol-5-yl]piperidin-1-yl]methanone |
| Canonical SMILES | C1CC(CN(C1)C(=O)C2=CC=C(C=C2)F)C3=NC(=NO3)C4=CC=C(C=C4)F |
| 分子式 | C20H17F2N3O2 |
| 分子量 | 369.36 |
| 溶解度 | DMF: 2 mg/mL,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml,Ethanol: 2 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | ADX-47273 is a potent and selective mGluR5 receptor PAM (positive allosteric modulator), EC50 = 0.17 μm, with no effect on other mGluR subtypes. [1] The mGluR (metabotropic glutamate receptor) is a group of G-protein coupled receptors and is active through an indirect metabotropic process. It plays a critical role in regulating synaptic plasticity and neural network activity. In HEK-293 cell expressing rat mGlu5, ADX-showed 9-fold higher response (EC50 = 0.17 μm) to threshold concentration of glutamate (50 nM) in the fluorometric Ca2+ assays, it also shifted mGlu5 receptor glutamate response curve to the left. [1] In vivo, ADX47273 increased ERK (extracellular signal-regulated kinase) and CREB (cAMP-responsive element-binding protein) phosphorylation in rat hippocampus and prefrontal cortex. In rat and mouse models that sensitive to antipsychotic treatment, ADX47273 decreased rat conditioned avoidance responding (minimal effective dose = 30 mg/kg i.p.) and reduced mouse ampomorphine-activated climbing (minimal effective dose = 100 mg/kg i.p.) [1] Reference: |
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