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ZD-1611
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ZD-1611图片
CAS NO:186497-38-1
规格:98%
分子量:456.51
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
ZD-1611是一种有效的,可口服的,选择性的ETAreceptor拮抗剂,可用于缺血性脑中风的研究。
CAS:186497-38-1
分子式:C22H24N4O5S
分子量:456.51
纯度:98%
存储:Store at -20°C

Background:

ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.


ZD1611 competitively inhibits 125I-labeled ET-1 binding at human cloned ETA and ETB receptors with pIC50 values of 8.6 and 5.6, respectively, showing 1000-fold selectivity for the ETA receptor[1].


ZD1611 (0.3 mg/kg, p.o.) has a duration of action of more than 7 h in rats. In the dog, ZD1611 is active for at least 6 h at dose of 0.6 mg/kg p.o[1]. ZD1611 (0.15 mg/kg/day) in combination with candesartan decreases the brain damage and improves the neurological scores in rats. However, ZD1611 or candesartan alone does not significantly decrease the brain damage or improve neurological scores[2].


[1]. Wilson C, et al. Pharmacological profile of ZD1611, a novel, orally active endothelin ETA receptor antagonist. J Pharmacol Exp Ther. 1999 Sep;290(3):1085-91. [2]. Stenman E, et al. Cooperative effect of angiotensin AT(1) and endothelin ET(A) receptor antagonism limits the brain damage after ischemic stroke in rat. Eur J Pharmacol. 2007 Sep 10;570(1-3):142-8. Epub 2007 Jun 9.