13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
聯系人:高小姐
電話:021-59541103 021-60443211
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Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 10mM (in 1mL DMSO) 5mg 10mg 50mg |
| CAS | 223104-29-8 |
| 別名 | SEA 0400;SEA-0400 |
| 化學名 | 2-[4-[(2,5-difluorophenyl)methoxy]phenoxy]-5-ethoxyaniline |
| 分子式 | C21H19F2NO3 |
| 分子量 | 371.38 |
| 溶解度 | ≥ 18.569 mg/mL in DMSO, ≥ 46.4 mg/mL in EtOH with ultrasonic |
| 儲存條件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice |
產品描述：
SEA0400 is a potent and selective inhibitor of Na+-Ca2+ exchanger (NCX) with IC50 values of 5 to 33 nM in cultured neurons, microglia and astrocytes [1].
The Na+-Ca2+ exchanger is an anti-porter that pumps Ca2+ out of the cells and keeps the low concentration of Ca2+ inside cells through exchanging the Na+ and Ca2+. In the reperfusion injury, the reverse mode NCX is activated, inducing the paradoxical Ca2+ influx and subsequently causing the generation of free radicals, leucotriene and thromboxane. Many existed drugs target NCX treated for reperfusion injury are reported of lacking selectivity or cell- permeability while SEA0400 is reported to be the most selective and potent NCX inhibitor [1].
SEA0400 was screened out of a chemical library designed for inhibition of NCX in cultured astrocytes and isolated cardiac sarcolemmal vesicles. It showed potent inhibitory effects on Na+-dependent Ca2+ uptake in cultured microglia, astrocytes and neurons with IC50 values of 8.3, 5 and 33 nM, respectively. The activity of SEA0400 was more than 100-fold higher than that of KB-R7943. SEA0400 was also proved to be selective against NCX over other ion fluxes since it displayed no significant effect on SOCE even at the concentration up to 3 μM. Besides that, SEA0400 had no effect on a serious of similar ion channels or ion transporters such as Ca2+-ATPase, Na+, K+-ATPase and K+ channel. Moreover, SEA0400 was found to suppress the Ca2+ influx-induced apoptosis in astrocytes [1].
In a rat model of cerebral ischemia, injection of SEA0400 at dose of 3 mg/kg resulted in decreased infarct volume in both striatum and cerebral cortex. In a rabbit model of Langendorff-perfused 1-month myocardial infarction, SEA0400 administration inhibited the pacing-induced ventricular premature beats and displayed proarrhythmic activity through enhancing spatially discordant alternans (SDA) and steepening Action potential duration (APD) restitution [1 and 2].
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原創作者：上海莼試生物技術有限公司
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賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業部
賬 號：2169 2341 6278
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