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Submit ReviewVU 0409551
说明： Selective positive allosteric modulator of mGlu5 receptors; brain penetrant and orally bioavailable
别名： JNJ 46778212
化学名： [6,7-Dihydro-2-(phenoxymethyl)oxazolo[5,4-c]pyridin-5(4H)-yl](fluorophenyl)methanone
纯度： ≥98% (HPLC)
生物活性 for VU 0409551
VU 0409551 is a 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.
化合物库 for VU 0409551
VU 0409551 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for VU 0409551
| 分子量 | 352.36 |
| 公式 | C20H17FN2O3 |
| 储存 | Store at +4°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1363281-27-9 |
| PubChem ID | 56846694 |
| InChI Key | QUZLMKNNIUSREV-UHFFFAOYSA-N |
| Smiles | O=C(C1=CC=C(F)C=C1)N(C2)CCC3=C2OC(COC4=CC=CC=C4)=N3 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for VU 0409551
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 35.24 | 100 | |
| ethanol | 17.62 | 50 |
制备储备液 for VU 0409551
以下数据基于产品分子量 352.36。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.84 mL | 14.19 mL | 28.38 mL |
| 5 mM | 0.57 mL | 2.84 mL | 5.68 mL |
| 10 mM | 0.28 mL | 1.42 mL | 2.84 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.57 mL |
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产品说明书 for VU 0409551
参考文献 for VU 0409551
参考文献是支持产品生物活性的出版物。
Rook et al (2015) Biased mGlu5-positive allosteric modulators provide in vivo efficacy without potentiating mGlu5 modulation of NMDAR currents. Neuron 86 1029 PMID: 25937172
Conde-Ceide et al (2015) Discovery of VU0409551/JNJ-46778212: An mGlu5 positive allosteric modulator clinical candidate targeting schizophrenia. ACS Med.Chem.Lett. 6 716 PMID: 26157544
Ghoshal et al (2017) Role of mGlu5 receptors and inhibitory neurotransmission in M1 dependent muscarinic LTD in the prefrontal cortex: implications in Schizophrenia. ACS Chem.Neurosci. 8 2254 PMID: 28679049
If you know of a relevant reference for VU 0409551, please let us know.
关键词: VU 0409551, VU 0409551 supplier, JNJ46778212, VU0409551, metabotropic, glutamate, receptors, mGlu5, positive, allosteric, modulators, modulates, PAMs, JNJ, 46778212, Glutamate, (Metabotropic), Group, I, Receptors, 5693, Tocris Bioscience
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该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
Metabotropic Glutamate Receptors Scientific Review
Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.
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