货号 | 5693/50 |
别名 | [6,7-Dihydro-2-(phenoxymethyl)oxazo |
供应商 | Tocris |
生物活性 | Selective mGlu5 positive allosteric modulator (EC50 = 260 nM). Selective for mGlu5 over other mGluR subtypes, as well as 66 other receptors and ion channels. Selectively potentiates mGlu5 signaling via Gαq. Exhibits wake-promoting, antipsychotic-like and cognition-enhancing effects in animal models. Brain penetrant and orally available. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >98 % |
计算分子量 | 352.36 |
分子式 | C20H17FN2O3< |
可溶性/溶解性 | Soluble to 100 mM in DMSO and to 50 mM in ethanol |
参考文献 | Conde-Ceideet al (2015) Discovery of VU0409551/JNJ-46778212: An mGlu5 positive allosteric modulator clinical candidate targeting schizophrenia. ACS Med.Chem.Lett. 6 716. PMID: 26157544. Rooket al (2015) Biased mGlu5-positive allosteric modulators provide in vivo efficacy without potentiating mGlu5 modulation of NMDAR currents. Neuron 86 1029. PMID: 25937172. |