产品
编 号：F194704
分子式：C28H26O9
分子量：506.5
分子式：C28H26O9
分子量：506.5
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CAS No: 162256-50-0
产品详情
生物活性：
CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration.
体内研究：
CI-1020 (30mg/kg， p.o.) 对 ET-A 完全抑制，并且不影响正常大鼠的基础血压。CI-1020f (40mg/kg，p.o.) 减轻暴露于慢性缺氧的大鼠中已建立的肺动脉高压。Animal Model:normal rats
Dosage:30 mg/kg
Administration:oral administration (p.o.)
Result:Inhibited the ET-A and has no significant effect on basal blood pressure in normotensive rats.
Animal Model:basal blood pressure in normotensive rats
Dosage:40 mg/kg/day
Administration:oral administration (p.o.)
Result:Reduced the increase in RV/LV+S and the percentage DEL induced by chronic hypoxia.Lowered the increase in pulmonary resistance in isolated perfused lungs significantly.
体外研究：
CI-1020 (1 μM， 28 天) 在器官培养中完全阻断人隐静脉内膜增生。CI-1020 (1 μM， 14 天) 对组织无毒。
CI-1020 (PD156707) is an orally active and selective antagonist targeting endothelin (ETA) with an IC50 value of 0.3 nM. CI-1020 blocks intimal hyperplasia in human saphenous veins completely in organ culture. CI 1020 inhibits hypoxic pulmonary hypertension and blocks ET-1-induced pressor responses following oral administration.
体内研究：
CI-1020 (30mg/kg， p.o.) 对 ET-A 完全抑制，并且不影响正常大鼠的基础血压。CI-1020f (40mg/kg，p.o.) 减轻暴露于慢性缺氧的大鼠中已建立的肺动脉高压。Animal Model:normal rats
Dosage:30 mg/kg
Administration:oral administration (p.o.)
Result:Inhibited the ET-A and has no significant effect on basal blood pressure in normotensive rats.
Animal Model:basal blood pressure in normotensive rats
Dosage:40 mg/kg/day
Administration:oral administration (p.o.)
Result:Reduced the increase in RV/LV+S and the percentage DEL induced by chronic hypoxia.Lowered the increase in pulmonary resistance in isolated perfused lungs significantly.
体外研究：
CI-1020 (1 μM， 28 天) 在器官培养中完全阻断人隐静脉内膜增生。CI-1020 (1 μM， 14 天) 对组织无毒。
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