SEA0400
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.
SEA0400是一种有效的和选择性的Na+-Ca2+交换体(NCX)抑制剂,在培养的神经元,小胶质细胞和星形胶质细胞中IC50范围介于5-33 nM之间,比KB-R7943的作用强100倍以上[1]。
Na+-Ca2+交换体是一种反向协同运输体系(anti-porter),通过Na+/Ca2+交换,细胞内的Ca2+外流,使细胞内保持低Ca2+浓度。在再灌注损伤中,反向NCX被激活,诱导Ca2+内流,随后引起自由基,白三烯和血栓素的产生。许多用于治疗再灌注损伤的靶向NCX的药物缺乏选择性或细胞通透性,而SEA0400是一个最具选择性的和有效的NCX抑制剂[1]。
SEA0400是从专门用于筛选NCX抑制剂的化合物库中获得的。SEA0400对NCX具有选择性,在浓度高达3 μM时,SEA0400对SOCE没有显著的效果。SEA0400对一些相似的离子通道或离子转运体也没有效果,例如Ca2+-ATPase、Na+,K+-ATPase和K+通道。SEA0400可以抑制星形胶质细胞中Ca2+内流诱导的细胞凋亡[1]。
在脑缺血大鼠模型中,SEA0400(3 mg/kg)可以减少纹状体和大脑皮层中的梗死体积。在Langendorff灌注1个月后诱导的心肌梗死兔模型中,SEA0400抑制起搏诱导的室性早搏,通过增强空間非同步电交替(spatially discordant alternans,SDA)和加快动作电位时程(action potential duration,APD)恢复,具有促心律失常的活性[1,2]。
参考文献:
[1] Matsuda T, Arakawa N, Takuma K, et al. SEA0400, a novel and selective inhibitor of the Na+-Ca2+ exchanger, attenuates reperfusion injury in the in vitro and in vivo cerebral ischemic models. Journal of Pharmacology and Experimental Therapeutics, 2001, 298(1): 249-256.
[2] CHOU C C, CHANG P O C, WEN M S, et al. Effects of SEA0400 on Arrhythmogenicity in a Langendorff-Perfused 1-Month Myocardial Infarction Rabbit Model Pacing and Clinical Electrophysiology, 2013, 36(5): 596-606.
- 1. Weizhen Li, Emilia Entcheva. "Syncytium cell growth increases IK1 contribution in human iPS-cardiomyocytes." bioRxiv. 2019 December 03.
- 2. Nie J, Duan Q, et al. "Ranolazine prevents pressure overload-induced cardiac hypertrophy and heart failure by restoring aberrant Na(+) and Ca(2+) handling." J Cell Physiol. 2018 Nov 29. PMID:30488495
- 3. Halty-deLeon L, Hansson BS, Wicher D. "The Drosophila melanogaster Na(+)/Ca(2+) Exchanger CALX Controls the Ca(2+) Level in Olfactory Sensory Neurons at Rest and After Odorant Receptor Activation." Front Cell Neurosci. 2018 Jul 3;12:186. PMID:30018538
- 4. Jovana Bojcevski, dipl. Phys. "Calcium-mediated mechanisms of retinal ganglion cell degeneration during autoimmune optic neuritis." Ruperto-Carola University of Heidelberg, Germany. 2017 May 23.
- 5. Hashad AM, Mazumdar N, et al. "Interplay among distinct Ca(2+) conductances drives Ca(2+) sparks/spontaneous transient outward currents in rat cerebral arteries." J Physiol. 2016 Nov 2. PMID:27805790
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 371.38 |
Cas No. | 223104-29-8 |
Formula | C21H19F2NO3 |
Synonyms | SEA 0400;SEA-0400 |
Solubility | insoluble in H2O; ≥18.57 mg/mL in DMSO; ≥46.4 mg/mL in EtOH with ultrasonic |
Chemical Name | 2-[4-[(2,5-difluorophenyl)methoxy]phenoxy]-5-ethoxyaniline |
SDF | Download SDF |
Canonical SMILES | CCOC1=CC(=C(C=C1)OC2=CC=C(C=C2)OCC3=C(C=CC(=C3)F)F)N |
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。 |
细胞实验[1]: | |
细胞系 |
皮质神经元(从18天的大鼠胎儿中分离)、星形胶质细胞和小胶质细胞(从1日龄Wistar大鼠的大脑皮层中分离)。 |
溶解方法 |
溶于DMSO。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
10 min;IC50:33 nM(神经元)、5.0 nM(星形胶质细胞)和8.3 nM(小胶质细胞)。 |
应用 |
SEA040是一种最有效的和选择性的Na+-Ca2+交换体(NCX)抑制剂,抑制Na+依赖的Ca2+吸收,IC50值分别为33 nM(神经元)、5.0 nM(星形胶质细胞)和8.3 nM(小胶质细胞)。 |
动物实验[2]: | |
动物模型 |
豚鼠 |
剂量 |
豚鼠用戊巴比妥钠(50 mg/kg;i.p.)麻醉,稳定15 min后,SEA0400以1–10 mg/kg的剂量(每只动物只接受一种剂量)通过颈静脉注射,5 min后,注射25 μg/kg的乌头碱(aconitine),诱发室性心律失常。 |
应用 |
SEA0400在10 mg/kg剂量时没有引起显著的变化,正常窦性心律、PVC、窄QRS VT和宽QRS VT的持续时间分别是21.5、4.3、17.3和16.8 min。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Matsuda T, Arakawa N, Takuma K, et al. SEA0400, a novel and selective inhibitor of the Na+-Ca2+ exchanger, attenuates reperfusion injury in the in vitro and in vivo cerebral ischemic models. Journal of Pharmacology and Experimental Therapeutics, 2001, 298(1): 249-256. [2] Amran M S, Hashimoto K, Homma N. Effects of sodium-calcium exchange inhibitors, KB-R7943 and SEA0400, on aconitine-induced arrhythmias in guinea pigs in vivo, in vitro, and in computer simulation studies. Journal of Pharmacology and Experimental Therapeutics, 2004, 310(1): 83-89. |
描述 | SEA0400是一种新型的和选择性的Na+-Ca2+交换体(NCX)抑制剂,IC50值为5-33 nM。 | |||||
靶点 | Na+-Ca2+ exchanger | |||||
IC50 | 5-33 nM |
质量控制和MSDS
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