PD123319

PD123319CAS号: 130663-39-7分子式: C31H32N4O3分子量: 508.61描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)

产品描述
描述

PD123319是一种有效的,选择性AT2血管紧张素Ⅱ受体拮抗剂, IC50为34 nM。

纯度
≥98%
储存/保存方法
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
基本信息
别名
PD123319; PD-123319; (S)-(+)-PD 123319
外观
powder
可溶性/溶解性
DMSO :100 mg/mL (196.61 mM)
Water :100 mg/mL (196.61 mM)
Ethanol :100 mg/mL (196.61 mM)
生物活性
靶点
AT2 receptor
In vitro(体外研究)
PD 123319 is shown to discriminate between two subclasses of AII receptors in many different tissues. 125I-AII specifically labeled two classes of binding sites for AII in a membrane preparation of bovine adrenal glomerulosa cells. The first class (DuP-753 sensitive) represents approximately 85% of the total binding sites for AII and possesses a high affinity (IC50 of 92.9 nM) for DuP-753. PD-123319 does not have any effect on 125I-AII binding to this site. The second class of binding sites is more sensitive to PD-123319, with an IC50 of 6.9 nM, and has a much lower affinity for DuP-753 (IC50 around 10 microM).
In vivo(体内研究)
PD 123319 has no effect on cerebral blood flow autoregulation. Acute AT2-receptor blockade does not influence CBF autoregulation. Intravenous administration of PD 123319 to conscious hypertensive rats elicites an immediate dose-dependent increase in MAP that is sustained for approximately 7.4 min with 3 mg/kg PD 123319.

分子结构图

PD123319