产品描述

PD 123319是有效的，选择性AT2血管紧张素Ⅱ受体拮抗剂，IC50 为34 nM。

靶点

AT2 angiotensin II receptor

IC50

34 nM

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).

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. [4] – See more at: http://www.selleckchem.com/products/pd123319.html#sthash.AZDud0GK.dpuf

溶解性

DMSO 100 mg/mL，水 100 mg/mL，乙醇 100 mg/mL

稳定性

2年 -20°C粉状，6月-80°C溶于DMSO

特征