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| 靶点 |
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| 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]. |
| 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. | |
| 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 |
| 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 |
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| 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 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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