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抑制剂描述:

产品名称:PD123319

产品别名:见爱必信官网

英文别名:PD123319

靶点:Angiotensin Receptor

CAS:130663-39-7

纯度:≥98%

外观:见爱必信官网

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.

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。

溶解性:DMSO :100 mg/mL (196.61 mM)
Water :100 mg/mL (196.61 mM)
Ethanol :100 mg/mL (196.61 mM)

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.

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