Products

Enzymes for Research, Diagnostic and Industrial Use

SEA0400

Cat No.
CEI-1525
Description
SEA0400 is a novel and selective inhibitor of the Na+-Ca2+ exchanger (NCX) with IC50 value of 5-33 nM.
Product Overview
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. 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. 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. 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.
CAS No.
223104-29-8
Molecular Weight
371.38
Purity
0.9975
Storage
Store at -20°C
Synonyms
SEA 0400; SEA-0400
Targets
NCX
IC50
5-33 nM
Molecular Formula
C21H19F2NO3
Chemical Name
2-[4-[(2,5-difluorophenyl)methoxy]phenoxy]-5-ethoxyaniline
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
Download Datasheet:



Inquiry
Online Inquiry
Name:
*Phone:
*E-mail Address:
Country:
Company/Institution:
*Products or Services Interested:
Quantity:
Project Description:
Our Products are Not Intended for Private Therapeutic Use!
*Verification Code:
Please input "enzymes"(case insensitive) as verification code.

Welcome! For price inquiries, please feel free to contact us through the form below through the form on the left side. We will get back to you as soon as possible.

Sitemap  Privacy Policy
Copyright ©2011 - 2017 Creative Enzymes.
Contact Us 45-1 Ramsey Road, Shirley, NY 11967, USA
Email: info@creative-enzymes.com
Tel: 1-631-562-8517 1-631-448-7888
Fax: 1-631-938-8127
Distributors To view the contact information for a specific location, select the desired country: