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 > ABT-546
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:
 
ABT-546
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。
ABT-546图片
CAS NO:212481-66-8
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
A-216546
产品介绍
ABT-546 (A-216546) 是一种有效的,高选择性和活性的内皮素ETA受体拮抗剂,对 [125I]-内皮素-1 与克隆的人ETA结合的Ki为 0.46 nM。ABT-546 对ETA的选择性比对 ETB受体的选择性高 25,000 倍以上。ABT-546 阻断内皮素-1 诱导的花生四烯酸释放和磷脂酰肌醇水解,IC50分别为 0.59 nM 和 3 nM。
生物活性

ABT-546 (A-216546) is a potent, highly selective and activeendothelinETAreceptorantagonist with aKiof 0.46 nM for [125I]endothelin-1 binding to clonedhuman endothelinETA. ABT-546 is >25,000-fold more selective for theETAreceptorthan for theETBreceptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis withIC50of 0.59 nM and 3 nM, respectively[1].

IC50& Target[1]

ETA

0.46 nM (Ki)

体外研究
(In Vitro)

ABT-546 (A-216546) effectively inhibits specific I endothelin-1 binding to endothelin ETAreceptor in membranes prepared from rat pituitary MMQ cells with an IC50value of 0.56 nM. ABT-546 is much less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETBrceptor in membranes prepared from porcine cerebellum with an IC50value of 16,700 nM. In membranes prepared from CHO cells stably transfected with the human endothelin ETAand ETBreceptors, ABT-546 again effectively inhibits specific [125I]endothelin-1 binding to endothelin ETAreceptor with an IC50value of 0.49 nM, but is less effective in inhibiting specific [125I]endothelin-3 binding to endothelin ETBreceptor with an IC50value of 15,400 nM[1].
In isolated vessels, ABT-546 inhibits endothelin ETAreceptor-mediated endothelin-1-induced vasoconstriction, and endothelin ETBreceptor-mediated sarafotoxin 6c-induces vasoconstriction with pA2of 8.29 and 4.57, respectively[1].

体内研究
(In Vivo)

ABT-546 (A-216546; 0-100 mg/kg; oral administration; for 1 hour or 4 hours; male Sprague-Dawley rats) treatment dose-dependently blocks endothelin-1-induced pressor response in conscious rats[1].

Animal Model:Male Sprague-Dawley rats (250-350 g) induced with endothelin-1[1]
Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
Administration:Oral administration; for 1 hour or 4 hours
Result:Exhibited a dose-dependent inhibition of the peak pressor response to endothelin-1, and statistically significant inhibition was achieved at doses of 3 to 100 mg/kg.
分子量

532.71

Formula

C30H48N2O6

CAS 号

212481-66-8

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.