您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > IRL-1620
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:
 
IRL-1620
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。
CAS NO:142569-99-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
IRL-1620 是高效,选择性的内啡肽受体 (endothelin receptor) B 型激动剂,Ki值为 16 pM。
生物活性

IRL-1620 is a potent and selectiveendothelin receptortype B (ETB)agonist with aKiof 16 pM.

IC50& Target

ETB

 

体外研究
(In Vitro)

IRL-1620 is the most potent and specific ligand for the ETB receptor (KiETA/ KiETB=120,000) as judged by the Kivalues for ETA (19 μM) and ETB (16 PM) receptors[1].
IRL-1620 is 60 times more selective for the ETB receptor than ET-3 (KiETA/ KiETB=1,900)[1].

体内研究
(In Vivo)

IRL-1620 (1-100 nM) induces contractions of the guinea pig trachea. The effective concentration that produces 30 % of 60 mM KCI-induced contraction is estimated to be 28 nM for IRL 1620[1].
IRL-1620 (1-100 nM) increases cytosolic Ca2+in the vascular endothelium ([Ca]E) with little effect on resting muscle tone, and relaxes the norepinephrine-stimulated tone with an increase in [Ca]E, in rat aorta,[1].
IRL-1620 improves both acquisition (learning) and retention (memory) on the water maze task and enhances angiogenic and neurogenic remodeling. Rats treated with IRL-1620 significantly reduces the cognitive impairment induced by Aβ. IRL-1620 treatment enhances the number of blood vessels labeled with VEGF compared to vehicle treatment[2].
IRL-1620, restores analgesic tolerance to morphine and oxycodone, but it does not affect morphine and oxycodone induced decrease in NGF/PI3K expression. IRL-1620 attenuates opioid tolerance without the involvement of NGF/PI3K pathway[3].

分子量

1820.95

Formula

C86H117N17O27

CAS 号

142569-99-1

Sequence

{Suc}-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp

Sequence Shortening

{Suc}-DEEAVYFAHLDIIW

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.