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Submit ReviewVU 6019650
说明： M5 receptor antagonist
化学名： (3R,4S)-rel-1-[(2,3-Dihydro-5-benzofuranyl)sulfonyl]-3-fluoro-4-[[(1-methyl-1H-imidazol-2-yl)thio]methyl]piperidine
纯度： ≥98% (HPLC)
生物活性 for VU 6019650
VU 6019650 is a potent and selective M5 receptor antagonist (hM5 IC50 = 36 nM). Exhibits >100-fold selectivity over human and rat M1-4. In vivo, VU 6019650 inhibits the reward effects of oxycodone and reduces oxycodone self-administration in rats. VU 6019650 is blood brain barrier penetrant.
许可信息
Sold under license from Vanderbilt University
技术数据 for VU 6019650
| 分子量 | 411.51 |
| 公式 | C18H22FN3O3S2 |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2926782-31-0 |
| PubChem ID | 164673826 |
| InChI Key | MWXZKSDFCSPEBK-ZBFHGGJFSA-N |
| Smiles | O=S(C1=CC=C(OCC2)C2=C1)(N3C[C@@H]([C@H](CC3)CSC4=NC=CN4C)F)=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.
溶解性数据 for VU 6019650
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 20.58 | 50 |
制备储备液 for VU 6019650
以下数据基于产品分子量 411.51。 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 |
|---|---|---|---|
| 0.5 mM | 4.86 mL | 24.3 mL | 48.6 mL |
| 2.5 mM | 0.97 mL | 4.86 mL | 9.72 mL |
| 5 mM | 0.49 mL | 2.43 mL | 4.86 mL |
| 25 mM | 0.1 mL | 0.49 mL | 0.97 mL |
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产品说明书 for VU 6019650
参考文献 for VU 6019650
参考文献是支持产品生物活性的出版物。
Garrison et al (2022) Development of VU6019650: a potent, highly selective, and systemically active orthosteric antagonist of the M5 muscarinic acetylcholine receptor for the treatment of opioid use disorder. J.Med.Chem. 65 6273 PMID: 35417155
Capstick et al (2022) Discovery of a potent M5 antagonist with improved clearance profile. Part 1: Piperidine amide-based antagonists. Bioorg.Med.Chem.Lett. 76 128988 PMID: 36113671
If you know of a relevant reference for VU 6019650, please let us know.
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关键词: VU 6019650, VU 6019650 supplier, VU6019650, acetylcholine, muscarinic, machrs, receptors, m5, Antagonist, antagonists, potent, selective, bbb, blood, brain, barrier, oxycodone, in, vivo, M5, Receptors, 8055, Tocris Bioscience
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