Trandolapril (RU44570) hydrochloride 是一种非巯基前体化合物,水解为活性双乙酰 (Trandolapril hydrochlorideat)。Trandolapril hydrochloride 是一种口服有效的血管紧张素转换酶(ACE)抑制剂,用于研究高血压和充血性心力衰竭 (CHF) 及心肌梗死 (MI)。
产品描述
Trandolapril (RU44570) hydrochloride is a nonsulfhydryl prodrug that is hydrolysed to the active diacid Trandolapril hydrochlorideat. Trandolapril hydrochloride is an orally active angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI) [1].
体内活性
Trandolapril hydrochloride (3 mg/kg/day; p.o.; 7 d) reduces renal fibrosis in obstructive nephropathy in mice, by inhibiting renal interstitial matrix expression and myofibroblast activation, decreasing renal proinflammatory cytokine RANTES and TNF-α level [2]. Trandolapril hydrochloride (0.3 mg/kg/day; p.o.; 4 weeks) improves arterial mechanics in rats, prevents arterial hypertrophy, collagen and cellular fibronectin accumulation [3]. randolapril (0.3 mg/kg/day; p.o.; 4 months) exhibits a chronic anti-hypertension effects in rats, results in blood pressure decreasing [3]. Trandolapril hydrochloride (0.25 mg/kg; p.o.; twice a day; 4 months) inhibits Atherosclerosis in the Watanabe Heritable Hyperlipidemic Rabbit [4]. Animal Model: UUD (unilateral ureteral obstruction) model in Male CD-1 mice (18-22 g) [2] Dosage: 3 mg/kg Administration: Oral gavage; daily, for 7 days Result: Resulted in renal interstitial matrix expression (including fibronectin, type I, and type III collagen) decreasing, and inhibited myofibroblast activation by surprising a-smooth muscle actin (a-SMA) expression, decreased the RANTES (regulated on activation, normal T cell expressed and secreted) and TNF-α level. Animal Model: SHR model (spontaneously hypertensive rats, 4-week-old) [3] Dosage: 0.3 mg/kg Administration: Oral gavage; daily for 4 weeks Result: Reduced collagen content in the aortic media and increased ariterial distensibility up to about 80%. Animal Model: Watanabe heritable hyperlipidemic rabbit (3 months old) [4] Dosage: 0.25 mg/kg Administration: Oral gavage; twice a day; 9 months Result: Decreased in atherosclerotic involvement of the intimal surface, and also decreased cholesterol content in descending thoracic aorta.
Cas No.
87725-72-2
分子式
C24H35ClN2O5
分子量
467
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years