PD-156707 

PD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist. PD-156707 binds to human ET-A and ET-B receptors with K_i values of 0.17 nM and 133.8 nM, respectively. PD-156707 shows reversal of established chronic hypoxic pulmonary hypertension in rats. PD-156707 can be used for the study of diseases associated with abnormal ET-A receptor activation, particularly pulmonary hypertension, stroke, and heart failure^[1][2].

PD-156707 抑制 Ltk 细胞中 ET-1 诱导的肌醇磷酸产生（IC₅₀ = 2.4 nM），并抑制兔肾动脉 VSMC 细胞中 ET-1 刺激的花生四烯酸释放（IC₅₀ = 1.1 nM）^[1]。
PD-156707 (0.1-10 μM) 使兔股动脉中 ET-1 刺激的收缩浓度-反应曲线右移^[1]。
PD-156707 (1 μM) 对人隐静脉横截面自发性新生内膜增生产生显著的抑制作用^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

PD-156707 (10-40 mg/kg，口服，每日) 以剂量依赖方式逆转大鼠中已建立的慢性缺氧性肺动脉高压，并减轻右心室肥厚^[1]。
PD-156707 (0.003-0.3 mg/kg/h，静脉输注，1 小时) 以剂量依赖方式抑制兔中 ET-1 诱导的肾血管阻力 (RVR) 增加^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

528.48

C₂₈H₂₅NaO₉

162412-70-6

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

• [1]. Andrew C. G. Uprichard, et al. PD- 156707: A Selective Endothelin-A Receptor Antagonist. Cardiovascular Drug Reviews Vol. 16, No. 2, pp. 89-104.

  [2]. D P Ignasiak, et al. Effects of endothelin ETA receptor antagonism with PD 156707 on hemodynamics and renal vascular resistance in rabbits. Eur J Pharmacol. 1997 Mar 5;321(3):295-300.  [Content Brief]