E-4031
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
作用于hERG的IC50为7.7 nM。
E-4031是一种阻断ATP敏感性钾通道的抗心律失常药。
ATP敏感性钾通道广泛分布于包括肌肉、胰腺β细胞和脑在内的组织中。其活性受腺嘌呤核苷酸调节，由ATP水平下降和ADP水平上升激活。因此，ATP敏感性钾通道将细胞代谢与膜兴奋性联系起来。
体外：据报道，E-4031可诱导EADs或TdP，并且这种诱导与复极化变异性的显著增加相关。此外，0.1 uM的E-4031能够显著延长周期长度、动作电位持续时间和去极化最大舒张电位。E-4031还可以减少动作电位的上行速度以及舒张期去极化率[1]。
体内：动物研究显示，0.01和0.1 mg/kg的E-4031可以提供有效的体外血浆浓度，以显著抑制Ikr，从而延迟超过舒张起始的复极化，导致机电耦合的反转，提供了一种理想的心律失常底物[2]。另一项研究发现，E-4031可以延长所有LV层的QT间期和ARI，虽然中期的延长幅度最大，特别是心动过缓期间[3]。
临床试验：到目前为止，E-4031仍处于临床前研究阶段。
参考文献：
[1]. Verheijck EE, et al. Effects of delayed rectifier current blockade by E-4031 on impulse generation in single sinoatrial nodal myocytes of the rabbit. Circ Res. 1995 Apr;76(4):607-15.
[2]. Izumi-Nakaseko H, et al. Effects of selective IKr channel blockade by E-4031 on ventricular electro-mechanical relationship in the halothane-anesthetized dogs. Eur J Pharmacol. 2014 Oct 5;740:263-70.
[3]. Izumi D, et al. Effects of bepridil versus E-4031 on transmural ventricular repolarization and inducibility of ventricular tachyarrhythmias in the dog. Pacing Clin Electrophysiol. 2010 Aug;33(8):950-9.
| Storage | Store at -20°C |
| M.Wt | 401.52 |
| Cas No. | 113558-89-7 |
| Formula | C21H27N3O3S |
| Solubility | insoluble in H2O; ≥103 mg/mL in DMSO; ≥9.66 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | N-(4-(1-(2-(6-methylpyridin-2-yl)ethyl)piperidine-4-carbonyl)phenyl)methanesulfonamide |
| SDF | Download SDF |
| Canonical SMILES | CC1=NC(CCN2CCC(C(C3=CC=C(NS(C)(=O)=O)C=C3)=O)CC2)=CC=C1 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
