货号:A132165
同义名:
咪达普利盐酸盐
/ TA-6366;Imidapril (hydrochloride)
Imidapril HCl是一种ACE抑制剂,IC50为2.6 nM,可用于治疗高血压及研究1型糖尿病、肾病和慢性心力衰竭。
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描述 | Angiotensin-converting enzyme (ACE) is responsible for the conversion of angiotensin I (ATI) to angiotensin II (ATII), which regulates blood pressure and is a key component of the renin-angiotensin-aldosterone system (RAAS) [4]. Imidapril hydrochloride (imidapril) is a long-acting, non-sulfhydryl angiotensin-converting enzyme (ACE) inhibitor, which has been used clinically in the treatment of hypertension, chronic congestive heart failure (CHF), acute myocardial infarction (AMI), and diabetic nephropathy [5]. After oral administration, imidapril is rapidly converted in the liver to its active metabolite imidaprilat. The plasma levels of imidaprilat gradually increase in proportion to the dose, and decline slowly. The time to reach the maximum plasma concentration (Tmax) is 2.0 h for imidapril and 9.3 h for imidaprilat. The elimination half-lives (t1/2) of imidapril and imidaprilat is 1.7 and 14.8 h, respectively [5]. In patients with hypertension, blood pressure was still decreased at 24 h after imidapril administration. The antihypertensive effect of imidapril was dose-dependent [5]. The maximal reduction of blood pressure and plasma ACE was achieved with imidapril, 10 mg once daily, and the additional effect was not prominent with higher doses. When administered to patients with AMI, imidapril improved left ventricular ejection fraction and reduced plasma brain natriuretic peptide (BNP) levels [5]. In patients with mild-to-moderate CHF [New York Heart Association (NYHA) functional class II–III], imidapril increased exercise time and physical working capacity and decreased plasma atrial natriuretic peptide (ANP) and BNP levels in a dose-related manner. In patients with diabetic nephropathy, imidapril decreased urinary albumin excretion [5]. |
Dose | Cat: 0.5 mg/kg - 5 mg/kg[2] (p.o.) Dog: 0.25 mg/kg[2] (p.o.) | ||||||||||||
Administration | p.o. | ||||||||||||
Pharmacokinetics |
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计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.26mL 0.45mL 0.23mL |
11.31mL 2.26mL 1.13mL |
22.63mL 4.53mL 2.26mL |
CAS号 | 89396-94-1 |
分子式 | C20H28ClN3O6 |
分子量 | 441.906 |
别名 | 咪达普利盐酸盐 ;TA-6366;Imidapril (hydrochloride);Imidapril HCl |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Inert atmosphere,Store in freezer, under -20°C |
溶解方案 |
DMSO: 50 mg/mL(113.15 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 50 mg/mL(113.15 mM),配合低频超声助溶 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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动物实验配方 |
PO 0.5% CMC-Na 38 mg/mL suspension |