您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > BQ-3020
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
BQ-3020
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。
BQ-3020图片
CAS NO:143113-45-5
包装:500ug
规格:98%
市场价:3572元
分子量:2006.32

产品介绍
ETB receptor agonist,potent and selective
CAS:143113-45-5
分子式:C96H140N20O25S
分子量:2006.32
纯度:98%
存储:Store at -20°C

Background:

BQ-3020 is a linear endothelin (ET) analog that is highly selective for ETB receptors. It displaces [125I] ET-1 binding to ETB receptors in porcine cerebellar membranes with an IC50 value of 0.2 nM [1].


ET-1, a 21-amino acid peptide, is one of known isoforms of endothelin (ET-1, ET-2, ET-3), it has strong vasoconstrictor and mitogenic activity. ETB receptor is one of endothelin receptors (i.e. ETA and ETB). ETB receptor has nearly the same affinity for all endothelin isoforms [2].


BQ-3020 displaced [125I] ET-1 binding to ETB receptors in porcine cerebellar membranes at a concentration 4,700 times lower than that to ETA receptors (selective to ET-1) on aortic vascular smooth muscle cells (IC50: 940 nM) [1].


In eight healthy men aged from 20-28 years, the local response of Sarafotoxin S6c (SFTX6c) (5 pmol/min) or BQ-3020 (50 pmol/min) to intra-arterial or intravenous infusion was assessed. Comparing these studies, there was no significant difference between baseline measurements. All the effects were just in the infused arm. Following intra-arterial infusion, both SFTX6c and BQ-3020 produced vasoconstriction indicated by the reduction in forearm blood flow (-25±7% and -27±7%, respectively). Following intravenous infusion, both SFTX6c and BQ-3020 produced a vein diameter reduction (-30±8% and -16±7%, respectively) [3].


参考文献:
[1].  Ihara M, Saeki T, Fukuroda T, et al. A novel radioligand [125I]BQ-3020 selective for endothelin (ETB) receptors. Life Sci., 1992, 51(6):PL47-52.
[2].  Seo B, Oemar BS, Siebenmann R, et al. Both ETA and ETB receptors mediate contraction to endothelin-1 in human blood vessels. Circulation, 1994, 89(3):1203-8.
[3].  Strachan FE, Crockett TR, Mills NL, et al. Constriction to ETB receptor agonists, BQ-3020 and sarafotoxin S6c, in human resistance and capacitance vessels in vivo. Br J Clin Pharmacol., 2000, 50(1):27-30.