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Submit ReviewVU 0071063 is a selective activator of SUR1 Kir6.2 channels and pancreatic β-cell KATP channels (EC50 = 7 μM and 0.3-10.3 μM, respectively). VU 0071063 inhibits insulin secretion in pancreatic β-cells by inducing hyperpolarization of β-cell membranes and reduces voltage-dependent calcium channel activation and Ca2+ influx. VU 0071063 is active in vivo and brain penetrant.
分子量 | 326.4 |
公式 | C18H22N4O2 |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 333415-38-6 |
PubChem ID | 590142 |
InChI Key | ZFZAIHKQJBMYLO-UHFFFAOYSA-N |
Smiles | CC(C)(C1=CC=C(CN2C=NC3=C2C(N(C)C(N3C)=O)=O)C=C1)C |
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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 1.63 | 5 |
以下数据基于产品分子量 326.4。 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 |
---|---|---|---|
0.05 mM | 61.27 mL | 306.37 mL | 612.75 mL |
0.25 mM | 12.25 mL | 61.27 mL | 122.55 mL |
0.5 mM | 6.13 mL | 30.64 mL | 61.27 mL |
2.5 mM | 1.23 mL | 6.13 mL | 12.25 mL |
参考文献是支持产品生物活性的出版物。
Raphemot et al (2014) Direct activation of β-cell KATP channels with a novel xanthine derivative. Mol.Pharmacol. 85 858 PMID: 24646456
Kharade et al (2019) Structure-activity relationships, pharmacokinetics, and pharmacodynamics of the Kir6.2/SUR1-specific channel opener VU0071063. J.Pharmacol.Exp.Ther. 370 350 PMID: 31201216
If you know of a relevant reference for VU 0071063, please let us know.
关键词: VU 0071063, VU 0071063 supplier, VU0071063, selective, activators, potassium, channels, SUR1, Kir6.2, pancreatic, beta, cell, b-cells, Inward, rectifier, Potassium, Channels, 7057, Tocris Bioscience
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