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Pivalopril (Pivopril) Sale

(Synonyms: 匹伏普利; Pivopril; RHC 3659(S)) 目录号 : GC32544

Pivalopril (Pivopril) 是一种新型的口服活性血管紧张素转换酶 (ACE) 抑制剂。

Pivalopril (Pivopril) Chemical Structure

Cas No.:81045-50-3

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1mg
¥2,184.00
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5mg
¥4,330.00
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10mg
¥7,380.00
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20mg
¥12,990.00
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产品描述

Pivalopril is a new orally active angiotensin converting enzyme (ACE) inhibitor.

Pivalopril is a new compound with a hindered sulfur group that has been compared to Captopril for oral angiotensin-converting enzyme (ACE) inhibition in rats and dogs and antihypertensive activity in rats. In separate groups of conscious normotensive rats, Pivalopril (0.03-1.0 mg/kg, orally [p.o.]) produces a dose-related antagonism of angiotensin I (AngI)-induced pressor effects. The ED50 for Pivalopril and Captopril is 0.1 mg/kg. In conscious normotensive dogs, Pivalopril (incremental doses of 0.01-1.0 mg/kg, p.o.) produces a dose-related antagonism of AngI pressor effects. The ED50 is 0.17 mg/kg for Pivalopril and 0.06 mg/kg for Captopril. At equieffective doses the two compounds have similar durations of action. In sodium-deficient, conscious spontaneously hypertensive rats (SHR), Pivalopril (1-100 mg/kg, p.o.) produces a dose-related reduction in mean arterial pressure. The potency and duration are similar to those of Captopril. In the sodium-replete SHR, 5 days of oral dosing with Pivalopril (100 mg/kg per day) decreases mean arterial pressure more effectively than Captopril (100 mg/kg per day). It is concluded that Pivalopril is a potent, orally effective ACE inhibitor and antihypertensive agent[2].

[1]. Burnier M, et al. RHC 3659: a new orally active angiotensin converting enzyme inhibitor in normal volunteers. Br J Clin Pharmacol. 1981 Dec;12(6):893-9. [2]. Wolf PS, et al. Angiotensin-converting enzyme inhibitory and antihypertensive activities of pivalopril (RHC 3659-(S)). Fed Proc. 1984 Apr;43(5):1322-5.

Chemical Properties

Cas No. 81045-50-3 SDF
别名 匹伏普利; Pivopril; RHC 3659(S)
Canonical SMILES O=C(O)CN(C1CCCC1)C([C@H](C)CSC(C(C)(C)C)=O)=O
分子式 C16H27NO4S 分子量 329.45
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.0354 mL 15.1768 mL 30.3536 mL
5 mM 0.6071 mL 3.0354 mL 6.0707 mL
10 mM 0.3035 mL 1.5177 mL 3.0354 mL
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Research Update

Pivalopril improves anti-cancer efficiency of cDDP in breast cancer through inhibiting proliferation, angiogenesis and metastasis

Biochem Biophys Res Commun 2020 Dec 17;533(4):853-860.PMID:33008601DOI:10.1016/j.bbrc.2020.07.059.

Breast cancer is the most common cancer type among female worldwide. Cisplatin (cDDP) is one of the most effective chemotherapies for the treatment of breast cancer. Nevertheless, there is an urgent requirement to reduce its systemic side effects and chemoresistance. In this present study, Pivalopril (PP), a clinically used antihypertensive drug, has been verified as a chemosensitizer that extremely improves the sensitivity of breast cancer cells to cDDP. PP treatment markedly promoted the capacity of cDDP to reduce the proliferation of breast cancer cells. The combination of PP and cDDP significantly induced apoptosis and inhibited vascular endothelial growth factor (VEGF) expression in breast cancer cells, accompanied with reduced angiogenesis. Furthermore, PP plus cDDP effectively reduced the cell migration and invasion in breast cancer cells. The in vivo studies confirmed that the anti-metastatic effect of cDDP was further improved by PP, as evidenced by the markedly decreased number of metastatic nodules in lungs. Moreover, we confirmed that PP combined with cDDP cooperatively suppressed tumor growth in breast cancer xenograft mouse models without extra toxicity. Together, the present study provided the first evidence that PP greatly sensitized breast cancer cells to cDDP without additional toxicity, and the synergistic effect may be mainly through cooperatively inhibiting proliferation, angiogenesis, metastasis, and inducing apoptotic cell death.

Angiotensin-converting enzyme inhibitory and antihypertensive activities of Pivalopril (RHC 3659-(S))

Fed Proc 1984 Apr;43(5):1322-5.PMID:6323222doi

Pivalopril (RHC 3659-(S); (S)-N-cyclopentyl-N-(2-methyl-3-pivaloylthiopropionyl) glycine) is a new compound with a hindered sulfur group that has been compared to captopril for oral angiotensin-converting enzyme (ACE) inhibition in rats and dogs and antihypertensive activity in rats. In separate groups of conscious normotensive rats, Pivalopril (0.03-1.0 mg/kg, orally [p.o.]) produced a dose-related antagonism of angiotensin I (AngI)-induced pressor effects. The ED50 for Pivalopril and captopril was 0.1 mg/kg. In conscious normotensive dogs, Pivalopril (incremental doses of 0.01-1.0 mg/kg, p.o.) produced a dose-related antagonism of AngI pressor effects. The ED50 was 0.17 mg/kg for Pivalopril and 0.06 mg/kg for captopril. At equieffective doses the two compounds had similar durations of action. In sodium-deficient, conscious spontaneously hypertensive rats (SHR), Pivalopril (1-100 mg/kg, p.o.) produced a dose-related reduction in mean arterial pressure. The potency and duration were similar to those of captopril. In the sodium-replete SHR, 5 days of oral dosing with Pivalopril, 100 mg/(kg . day), decreased mean arterial pressure more effectively than captopril, 100 mg/(kg . day). No tolerance developed to the antihypertensive effect of either drug. It is concluded that Pivalopril is a potent, orally effective ACE inhibitor and antihypertensive agent.