186497-38-1
186497-38-1 結(jié)構(gòu)式
基本信息
中文別名
化合物 T17287 英文別名
ZD-1611Benzenepropanoic acid, 4-[3-[[(3-methoxy-5-methyl-2-pyrazinyl)amino]sulfonyl]-2-pyridinyl]-α,α-dimethyl-
物理化學(xué)性質(zhì)
沸點(diǎn)653.9±65.0 °C(Predicted)
密度1.339±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)4.62±0.13(Predicted)
常見(jiàn)問(wèn)題列表
生物活性
ZD-1611 是一種有效的，可口服的，選擇性的 ETA receptor 拮抗劑，可用于缺血性腦中風(fēng)的研究。體外研究
ZD1611 competitively inhibits 125 I-labeled ET-1 binding at human cloned ETA and ETB receptors with pIC 50 values of 8.6 and 5.6, respectively, showing 1000-fold selectivity for the ETA receptor.
體內(nèi)研究
ZD1611 (0.3 mg/kg, p.o.) has a duration of action of more than 7 h in rats. In the dog, ZD1611 is active for at least 6 h at dose of 0.6 mg/kg p.o. ZD1611 (0.15 mg/kg/day) in combination with candesartan decreases the brain damage and improves the neurological scores in rats. However, ZD1611 or candesartan alone does not significantly decrease the brain damage or improve neurological scores.