333415-38-6|VU0071063|CsnPharm

CAS No.: 333415-38-6

VU0071063 Catalog No. CSN29561

VU0071063 can activate native Kir6.2/SUR1 channels, thereby inhibiting glucose-stimulated calcium entry in isolated mouse pancreatic β cells.

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400-920-2911

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技术信息

生物活性

描述ATP sensitive potassium (K(ATP)) channels have important functions in neuroendocrine tissue, in smooth and skeletal muscle and in the heart. In pancreatic beta cells the K(ATP) channels, which are formed by 4 ion channels (Kir6.2) and 4 regulatory sulfonylurea receptors (SUR1), control the glucose stimulated release of insulin. The Kir6.2/SUR1 K(ATP) channels are also present in the brain and in other neuroendocrine tissues^[1]. KATP channel subunits expressed in rat liver and the diversity of KATP channel subunit composition might form different types of KATP channels. This is applicable to hepatocytes, HSCs, various types of Kupffer cells and sinusoidal endothelial cells^[2]. VU0071063 is a potent and specific Kir6.2/SUR1 opener (EC50=7.44 μM) and can be used for investigating Kir6.2/SUR1 expressed in the pancreas and brain. VU0071063 inhibits insulin secretion by inducing hyperpolarization of β-cell membrane potential^[3]. VU0071063 (1 nM~1 mM; HEK-293 cells) dose dependently opens Kir6.2/SUR1. VU0071063 (0~20 μM; isolated cells) inhibits β-Cell excitability in mouse Islets. VU0071063 (10 μM; 1 hour; isolated cells) inhibits glucose-stimulated insulin secretion. VU0071063 dose dependently and reversibly hyperpolarizes the β-cell membrane potential, which, in turn, inhibits glucose-stimulated Ca2+ entry and insulin secretion. The actions of VU0071063 on the β-cell membrane potential are reversed by tolbutamide, and glucose stimulated insulin secretion is unaffected by the inactive analog 34MT, indicating that the effects are mediated through Kir6.2/SUR1. VU0071063 (50 mg/kg; i.p.; 4 hours) leads to a significant increase in blood glucose at 60 minutes^[4].
参考文献

[1] John Bondo Hansen. Towards selective Kir6.2/SUR1 potassium channel openers, medicinal chemistry and therapeutic perspectives. Curr Med Chem. 2006;13(4):361-76.
[2] Ming Zhou,et al. Localization of ATP-sensitive K + channel subunits in rat liver. World J Exp Med. 2019 Dec 19;9(2):14-31.
[3] Raphemot R, et al. Direct activation of β-cell KATP channels with a novel xanthine derivative. Mol Pharmacol. 2014;85(6):858-865.
[4] Kharade SV, et al. Structure-Activity Relationships, Pharmacokinetics, and Pharmacodynamics of the Kir6.2/SUR1-Specific Channel Opener VU0071063. J Pharmacol Exp Ther. 2019;370(3):350-359.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.0638 mL
- 15.3190 mL
- 30.6379 mL
- 5 mM
- 0.6128 mL
- 3.0638 mL
- 6.1276 mL
- 10 mM
- 0.3064 mL
- 1.5319 mL
- 3.0638 mL

技术信息

CAS号	333415-38-6	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C18H22N4O2	运输	蓝冰
分子量	326.39	别名

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