P1075
目录号 : GC16848
P1075是一种有效的、磺酰脲受体2相关的ATP敏感性的钾通道(SUR2-KIR6) 的激活剂,EC50值为45±10nM。
Cas No.:60559-98-0
Sample solution is provided at 25 µL, 10mM.
P1075 is a potent activator of sulfonylurea receptor 2-related ATP-sensitive potassium channel (SUR2-KIR6) with an EC50 value of 45±10nM[1]. P1075 is a cyanoguanidine derivative that can increase anterior segment outflow capacity and reduce intraocular pressure[2]. P1075 can induce dilation of rat renal arteries[3]. P1075 can relax smooth muscle and shorten cardiac action potential duration (APD) in the nanomolar concentration range[4].
In vitro, P1075 (100μM) treatment of rabbit cardiomyocytes for 10min significantly induced the generation of intracellular ROS[5]. P1075 (30μM) treatment of rabbit ventricular myocytes significantly inhibited diazoxide-induced flavoprotein oxidation[6].
In vivo, P1075 (1μg/kg) treated by intravenous injection in rats with cardiac ischemia/reperfusion model significantly reduced the infarct size[7].
References:
[1] Schwanstecher M, Sieverding C, Dörschner H, et al. Potassium channel openers require ATP to bind to and act through sulfonylurea receptors[J]. The EMBO journal, 1998.
[2] Chowdhury U R, Bahler C K, Hann C R, et al. ATP-sensitive potassium (KATP) channel activation decreases intraocular pressure in the anterior chamber of the eye[J]. Investigative ophthalmology & visual science, 2011, 52(9): 6435-6442.
[3] Novakovic A, Pavlovic M, Milojevic P, et al. Different potassium channels are involved in relaxation of rat renal artery induced by P 1075[J]. Basic & clinical pharmacology & toxicology, 2012, 111(1): 24-30.
[4] Sargent C A, Sleph P G, Dzwonczyk S, et al. Cardioprotective effects of the cyanoguanidine potassium channel opener P-1075[J]. Journal of cardiovascular pharmacology, 1993, 22(4): 564-576.
[5] Oldenburg O, Yang X M, Krieg T, et al. P1075 opens mitochondrial KATP channels and generates reactive oxygen species resulting in cardioprotection of rabbit hearts[J]. Journal of molecular and cellular cardiology, 2003, 35(9): 1035-1042.
[6] Sato T, Nakaya H. P-1075 exerts diverse modulatory effects on mitochondrial ATP-sensitive K+ channels in rabbit ventricular myocytes[J]. Journal of cardiovascular pharmacology, 2006, 47(2): 165-168.
[7] Gross E R, Hsu A K, Gross G J. GSK3β inhibition and K ATP channel opening mediate acute opioid-induced cardioprotection at reperfusion[J]. Basic research in cardiology, 2007, 102: 341-349.
P1075是一种有效的、磺酰脲受体2相关的ATP敏感性的钾通道(SUR2-KIR6) 的激活剂,EC50值为45±10nM[1]。P1075是一种氰基胍衍生物,能够增加眼前节的流出能力,降低眼压[2]。P1075能够诱导大鼠肾动脉舒张[3]。P1075在纳摩尔浓度范围内可松弛平滑肌并缩短心肌动作电位持续时间(APD)[4]。
在体外,P1075(100μM)处理兔心肌细胞10min,显著诱导了细胞内ROS的生成[5]。P1075(30μM)处理兔心室肌细胞,显著抑制了二氮嗪诱导的黄素蛋白氧化[6]。
在体内,P1075(1μg/kg)通过静脉注射治疗心脏缺血/再灌注模型大鼠,显著减小了梗死面积[7]。
Cell experiment [1]: | |
Cell lines | Rabbit cardiomyocytes |
Preparation Method | Rabbit ventricular myocytes were isolated by collagenase perfusion. Experiments were performed 2-4d after isolation. Each experiment started with a change of medium for 10min. The medium was then removed and replaced with fresh medium containing the drug, and reduced MitoTracker™Reddye (500nM). Concentration of P1075 was 100µM, the incubation medium during the initial 10min of stabilization contained the blocker GLI (50µM) or 5HD (1mM). Incubating cells were stored at 37°C in the incubator. At the end of the 15min staining period, cells were washed two times with fresh MTR-free medium. Mitochondrial ROS generation was analyzed by measuring the fluorescence of 15-30 rod-shaped cells that were randomly selected within each well of the four-well chambers. |
Reaction Conditions | 100μM; 10min |
Applications | Fluorescence was markedly increased in cells treated with P1075 compared to controls. This P1075-induced ROS generation was abolished byco-incubation with the mitoKATP blocker 5HD. We also studied the effect of the non-selective, but potent, KATP blocker GLI on the P1075 response. P1075 again led to a robust and significant increase in ROS production. |
References: |
Cas No. | 60559-98-0 | SDF | |
化学名 | |||
Canonical SMILES | N#CN/C(NC1=CC=CN=C1)=N\C(C)(C)CC | ||
分子式 | C12H17N5 | 分子量 | 231.3 |
溶解度 | DMSO: <100mM,Ethanol: <50mM | 储存条件 | Store at RT |
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1 mg | 5 mg | 10 mg |
1 mM | 4.3234 mL | 21.6169 mL | 43.2339 mL |
5 mM | 0.8647 mL | 4.3234 mL | 8.6468 mL |
10 mM | 0.4323 mL | 2.1617 mL | 4.3234 mL |
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