Pivalopril (Pivopril)
(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。
Cas No.:81045-50-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
| 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 | DMSO : 90 mg/mL (273.18 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 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。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
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.