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Submit ReviewVU 0424465
Discontinued Product
6895 has been discontinued.
View all Glutamate (Metabotropic) Group I Receptors products.
说明： Potent mGlu5 positive allosteric modulator and agonist; binds allosteric site with high affinity
化学名： 5-[2-(2-(3-Fluorophenyl)ethynyl]-N-[(1R)-2-hydroxy-1,2-dimethylpropyl]-2-pyridinecarboxamide
纯度： ≥98% (HPLC)
生物活性 for VU 0424465
VU 0424465 is a potent mGlu5 positive allosteric modulator (EC50 = 1.5 nM) and agonist (EC50 = 171 nM; maximum effect is 65% that of glutamate). Binds allosteric site with high affinity (Ki = 11.8 nM). Increases maximum response to glutamate by 30%. Exhibits bias towards signaling via IP1 and ERK1/2 over iCa2+ in HEK293 and neuronal cells, and activates Gs in HEK 293 cells. Induces epileptiform activity in CA3 hippocampal neurons in vitro and convulsions in vivo.
技术数据 for VU 0424465
| 分子量 | 326.37 |
| 公式 | C19H19FN2O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1428630-85-6 |
| PubChem ID | 53384864 |
| InChI Key | ZPKZAFDYFVJULO-CYBMUJFWSA-N |
| Smiles | C[C@H](C(C)(O)C)NC(C1=CC=C(C#CC2=CC(F)=CC=C2)C=N1)=O |
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.
产品说明书 for VU 0424465
参考文献 for VU 0424465
参考文献是支持产品生物活性的出版物。
Rook et al (2013) Unique signaling profiles of positive allosteric modulators of metabotropic glutamate receptor subtype 5 determine differences in in vivo activity. Biol.Psychiatry. 73 501 PMID: 23140665
Sengmany et al (2017) Biased allosteric agonism and modulation of metabotropic glutamate receptor 5: Implications for optimizing preclinical neuroscience drug discovery. Neuropharmacology 115 60 PMID: 27392634
Nasrallah et al (2018) Direct coupling of detergent purified human mGlu5 receptor to the heterotrimeric G proteins Gq and Gs. Sci.Rep. 8 4407 PMID: 29535347
关键词: VU 0424465, VU 0424465 supplier, VU0424465, metabotropic, glutamate, receptor, subtype, 5, mGlu5, mGluR, agonist, positive, allosteric, modulators, modulates, agonists, agonism, potent, high, affinity, Glutamate, (Metabotropic), Group, I, Receptors, 6895, 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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