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Submit ReviewVU 6001966
说明： Potent and selective negative allosteric modulator of mGlu2 receptors
纯度： ≥98% (HPLC)
生物活性 for VU 6001966
VU 6001966 is a potent and selective mGlu2 negative allosteric modulator (IC50 = 78 nM). Exhibits > 350-fold selectivity for mGlu2 over mGlu3. Also exhibits selectivity over other mGluRs and a panel of GPCRs, ion channels and transporters. VU 6001966 induces antidepression like effects in mouse models of chronic stress. CNS penetrant.
许可信息
Sold under license from Vanderbilt University
化合物库 for VU 6001966
VU 6001966 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 6001966
| 分子量 | 326.33 |
| 公式 | C17H15FN4O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2009052-76-8 |
| PubChem ID | 122539788 |
| InChI Key | SSSNPJKQBYVHBV-UHFFFAOYSA-N |
| Smiles | CN1C=CC(COC2=CN=C(C(N)=O)C=C2C3=CC=C(C=C3)F)=N1 |
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 6001966
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 32.63 | 100 | |
| ethanol | 1.63 | 5 |
制备储备液 for VU 6001966
以下数据基于产品分子量 326.33。 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 | 3.06 mL | 15.32 mL | 30.64 mL |
| 5 mM | 0.61 mL | 3.06 mL | 6.13 mL |
| 10 mM | 0.31 mL | 1.53 mL | 3.06 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
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产品说明书 for VU 6001966
参考文献 for VU 6001966
参考文献是支持产品生物活性的出版物。
Bollinger et al (2017) Design and synthesis of mGlu2 NAMs with improved potency and CNS penetration based on a truncated picolinamide core. ACS Med.Chem.Lett. 8 919 PMID: 28947937
Joffe et al (2020) mGlu 2 and mGlu 3 negative allosteric modulators divergently enhance thalamocortical transmission and exert rapid antidepressant-like effects. Neuron 105 46 PMID: 31735403
If you know of a relevant reference for VU 6001966, please let us know.
关键词: VU 6001966, VU 6001966 supplier, VU6001966, metabotropic, glutamate, receptors, mGlu2, mGluR, mGlu2R, potent, selective, negative, allosteric, modulators, modulates, NAMs, CNS, penetrant, Glutamate, (Metabotropic), Group, II, Receptors, 6928, Tocris Bioscience
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