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SEA0400 {[allProObj[0].p_purity_real_show]}

货号:A527418

SEA0400是一种新型选择性的Na+-Ca2+交换器(NCX)抑制剂,抑制培养的神经元、星形胶质细胞和小胶质细胞中的Na+依赖性Ca2+摄取,IC50范围为5到33 nM。

SEA0400 化学结构 CAS号:223104-29-8
SEA0400 化学结构
CAS号:223104-29-8
SEA0400 3D分子结构
CAS号:223104-29-8
SEA0400 化学结构 CAS号:223104-29-8
SEA0400 3D分子结构 CAS号:223104-29-8
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SEA0400 纯度/质量文件 产品仅供科研

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SEA0400 生物活性

靶点
  • Calcium Channel

    NCX, IC50:33 nM

描述 SEA0400 is a novel and selective inhibitor of the Na+-Ca2+ exchanger (NCX), inhibiting Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50s of from 5 to 33 nM. Furthermore, administration of SEA0400 reduced infarct volumes after a transient middle cerebral artery occlusion in rat cerebral cortex and striatum[3]. SEA0400 at 0.3-1.0 microM protected microglia against SNP(Sodium nitroprusside)-induced apoptosis[4]. SEA0400 protects against MPTP-induced neurotoxicity probably by blocking ERK phosphorylation and lipid peroxidation which are downstream of NCX-mediated Ca(2+) influx[5]. The effects of SEA0400 on Ca2+ transient amplitude and the occurrence of spontaneous Ca2+ transients as a proxy measure for inotropy and cellular proarrhythmia depend on the NCX expression level[6].

SEA0400 细胞实验

Cell Line
Concentration Treated Time Description References
Platelets 2 µM 3 minutes SEA0400 reduced the collagen-induced increase in [Ca2+]i Br J Pharmacol. 2012 Feb;165(4):922-36.
Rat microglia 0.3–1.0 µM 12 hours SEA0400 attenuated SNP-induced apoptosis via suppression of the ER stress in cultured microglia. Br J Pharmacol. 2005 Mar;144(5):669-79.
Cardiomyocytes 1 µM 15 minutes SEA0400 prevented the lengthening of action potential induced by artemether Br J Pharmacol. 2020 Oct;177(19):4448-4463.
HEK293T cells 10 µM 30 minutes To evaluate the inhibitory effect of SEA0400 on NCX1.3 activity, results showed that SEA0400 significantly blocked the reverse mode activity of NCX1.3. EMBO J. 2024 Jan;43(1):14-31.
Guinea-pig ventricular myocytes 1 µM SEA0400 significantly inhibited the NCX current and had no significant effect on Na+, Ca2+, and K+ channels Br J Pharmacol. 2002 Mar;135(5):1096-100.
Canine ventricular myocytes 1 µM SEA0400 significantly inhibited both reverse and forward mode activities of NCX, but did not influence APD, CaT, or cell shortening. Br J Pharmacol. 2014 Dec;171(24):5665-81.
Pak1−/− atrial myocytes 1 µM Inhibited NCX activity, reduced spontaneous Ca2+ transients Heart Rhythm. 2018 Aug;15(8):1233-1241.
Rat ventricular cardiomyocytes 0.1, 0.3, 1.0 µM SEA0400 inhibited INa/Ca and exerted a positive inotropic effect in rat cardiomyocytes Br J Pharmacol. 2008 May;154(1):93-104.
Rabbit ventricular cardiomyocytes 0.1, 0.3, 1.0 µM SEA0400 inhibited INa/Ca but did not significantly affect contractility in rabbit cardiomyocytes Br J Pharmacol. 2008 May;154(1):93-104.

SEA0400 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats and rabbits Isolated Langendorff-perfused hearts Perfusion 0.1, 0.3, 1.0 µM Single administration SEA0400 exerted a concentration-dependent positive inotropic effect in rat hearts but had no significant effect in rabbit hearts Br J Pharmacol. 2008 May;154(1):93-104.
Mice Neonatal mouse ventricular myocardium 10 µM SEA0400 had no effect on the α-adrenoceptor-mediated positive inotropy Int J Mol Sci. 2023 Feb 15;24(4):3926

SEA0400 参考文献

[1]Nashida T, Takuma K, et al. The specific Na(+)/Ca(2+) exchange inhibitor SEA0400 prevents nitric oxide-induced cytotoxicity in SH-SY5Y cells. Neurochem Int. 2011 Aug;59(1):51-8.

[2]Matsuda T, Arakawa N, 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. J Pharmacol Exp Ther. 2001 Jul;298(1):249-56.

[3]Matsuda T, Arakawa N, Takuma K, Kishida Y, Kawasaki Y, Sakaue M, Takahashi K, Takahashi T, Suzuki T, Ota T, Hamano-Takahashi A, Onishi M, Tanaka Y, Kameo K, Baba A. SEA0400, a novel and selective inhibitor of the Na+-Ca2+ exchanger, attenuates reperfusion injury in the in vitro and in vivo cerebral ischemic models. J Pharmacol Exp Ther. 2001 Jul;298(1):249-56

[4]Nagano T, Osakada M, Ago Y, Koyama Y, Baba A, Maeda S, Takemura M, Matsuda T. SEA0400, a specific inhibitor of the Na+-Ca2+ exchanger, attenuates sodium nitroprusside-induced apoptosis in cultured rat microglia. Br J Pharmacol. 2005 Mar;144(5):669-79

[5]Ago Y, Kawasaki T, Nashida T, Ota Y, Cong Y, Kitamoto M, Takahashi T, Takuma K, Matsuda T. SEA0400, a specific Na+/Ca2+ exchange inhibitor, prevents dopaminergic neurotoxicity in an MPTP mouse model of Parkinson's disease. Neuropharmacology. 2011 Dec;61(8):1441-51

[6]Bögeholz N, Schulte JS, Kaese S, Bauer BK, Pauls P, Dechering DG, Frommeyer G, Goldhaber JI, Kirchhefer U, Eckardt L, Pott C, Müller FU. The Effects of SEA0400 on Ca2+ Transient Amplitude and Proarrhythmia Depend on the Na+/Ca2+ Exchanger Expression Level in Murine Models. Front Pharmacol. 2017 Sep 21;8:649

SEA0400 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.69mL

0.54mL

0.27mL

13.46mL

2.69mL

1.35mL

26.93mL

5.39mL

2.69mL

SEA0400 技术信息

CAS号223104-29-8
分子式C21H19F2NO3
分子量 371.38
SMILES Code NC1=CC(OCC)=CC=C1OC2=CC=C(OCC3=CC(F)=CC=C3F)C=C2
MDL No. MFCD07772188
别名
运输蓝冰
InChI Key YSUBLPUJDOWYDP-UHFFFAOYSA-N
Pubchem ID 644100
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

DMSO: 30 mg/mL(80.78 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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