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Submit ReviewVU 6005649
说明： Positive allosteric modulator of mGlu7 and mGlu8 receptors; also NK1 antagonist; brain penetrant
化学名： 3-(2,3-Difluoro-4-methoxyphenyl)-2,5-dimethyl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine
纯度： ≥98% (HPLC)
生物活性 for VU 6005649
VU 6005649 is a positive allosteric modulator of mGlu7 and mGlu8 receptors (EC50 = 0.65 μM and 2.6 μM for mGlu7 and mGlu8, respectively). Displays >3.8 fold selectivity for mGlu7 and mGlu8 over other mGlu receptors (EC50 >10 μM for mGlu1,2,3,4,5,6). Also NK1 receptor antagonist (Ki= 650 nM, IC50 = 3.4 μM). Brain penetrant.
化合物库 for VU 6005649
VU 6005649 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 6005649
| 分子量 | 357.28 |
| 公式 | C16H12F5N3O |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2137047-43-7 |
| PubChem ID | 131954513 |
| InChI Key | NYBZCKAQIIPSDS-UHFFFAOYSA-N |
| Smiles | COC1=C(F)C(F)=C(C=C1)C1=C2N=C(C)C=C(N2N=C1C)C(F)(F)F |
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 6005649
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 35.73 | 100 | |
| ethanol | 17.86 | 50 |
制备储备液 for VU 6005649
以下数据基于产品分子量 357.28。 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 | 2.8 mL | 13.99 mL | 27.99 mL |
| 5 mM | 0.56 mL | 2.8 mL | 5.6 mL |
| 10 mM | 0.28 mL | 1.4 mL | 2.8 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
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产品说明书 for VU 6005649
参考文献 for VU 6005649
参考文献是支持产品生物活性的出版物。
Abe et al (2017) Discovery of VU6005649, a CNS penetrant mGlu7/8 receptor PAM derived from a series of pyrazolo[1,5-a]pyrimidines. ACS.Med.Chem.Lett. 8 1110 PMID: 29057060
If you know of a relevant reference for VU 6005649, please let us know.
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关键词: VU 6005649, VU 6005649 supplier, VU6005649, positive, allosteric, modulators, modulates, PAM, metabotropic, glutamate, receptor, 7, 8, group, III, mGlu, neurokinin, 1, antagonists, antagonism, tachykinin, NK1, Glutamate, (Metabotropic), Group, Receptors, Receptor, 6893, 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。
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