标签归档：普利

Perindopril (Synonyms: 培哚普利; S-9490)

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Perindopril  (Synonyms: 培哚普利; S-9490) 纯度: 98.01%

Perindopril erbumine 是一种血管紧张素转换酶 (angiotensin-converting enzyme) 抑制剂，调节NF-κB 和 STAT3 信号传导，抑制胶质细胞活化和神经炎症，可用于慢性肾脏病和高血压的研究。

Perindopril (Synonyms: 培哚普利; S-9490)

Perindopril Chemical Structure

CAS No. : 82834-16-0

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生物活性

Perindopril erbumine is an angiotensin-converting enzyme inhibitor. Perindopril erbumine modulates NFκB and STAT3 signaling and inhibits glial activation and neuroinflammation. Perindopril erbumine can be used for the research of Chronic Kidney Disease and high blood pressure[1][2][3][4].

IC50 & Target

STAT3

 

SIRT3

 

体外研究
(In Vitro)

Perindopril erbumine (1 μM, 24 h) 改善 LPS (HY-D1056) 诱导的大鼠星形细胞瘤细胞系 (C6) 和小鼠小胶质细胞系(BV2) 中 AT2R 表达的减少和胶质增[1]。
Perindopril erbumine (1 μM, 24 h) 抑制LPS (HY-D1056) 诱导的大鼠星形细胞瘤细胞系 (C6) 和小鼠小胶质细胞系(BV2)中 IκBα 降解，NF кB 核转位和 STAT3 活化[1]。
Perindopril erbumine (1 μM, 24 h) 改善LPS (HY-D1056) 诱导的大鼠星形细胞瘤细胞系 (C6) 和小鼠小胶质细胞系(BV2) 中炎症因子释放失衡，抑制活性氧生成和亚硝酸盐释放[1]。

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Perindopril 相关抗体:
体内研究
(In Vivo)

Perindopril erbumine (0.1 mg/kg, Oral gavage, once a day for five consecutive days) prevents LPS-induced neuroinflammation in rats[1].
Perindopril erbumine (0.42 mg/kg, Oral, once a day for 4 weeks) with Huangqi-Danshen decoction (HDD) (4.7 g/kg, Oral, once a day for 4 weeks) attenuates adenine-induced Chronic kidney disease (CKD) in rats[2].
Perindopril erbumine (0.4-1.5 mg/kg, Oral, once a day for 4-24 weeks) has a persistent effect on blood pressure in spontaneously hypertensive rats (SHR)[4].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: LPS-induced neuroinflammation rat model[1]
Dosage: 0.1 mg/kg
Administration: Oral gavage (p.o.)
Result: Abolished the LPS-induced astroglial and microglial activation.
Attenuated LPS-induced TNF-α production.
Prevented LPS-induced nuclear translocation of NF-кB.
Prevented the AT1R up-regulation and the LPS-induced decrease in the expression of PP2A.
Animal Model: Adenine-induced chronic kidney disease rats[2]
Dosage: 0.42 mg/kg
Administration: Oral
Result: Obviously reduced serum creatinine (Scr) and blood urea nitrogen (BUN) levels.
Displayed a marked reduction of tubulointerstitial fibrosis.
Exhibited more inhibitory effect on Col-IV expression and a exceed effect of raising OPA-1 expression.
Significantly increased Sirtuin3 expression.
Prevented mitochondrial fragmentation.

Clinical Trial

分子量

368.47

Formula

C19H32N2O5
CAS 号

82834-16-0
性状

固体

颜色

Off-white to light yellow

中文名称

培哚普利
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O 中的溶解度 : 100 mg/mL (271.39 mM; 超声助溶 (<80°C))

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浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7139 mL 13.5696 mL 27.1392 mL
5 mM 0.5428 mL 2.7139 mL 5.4279 mL
10 mM 0.2714 mL 1.3570 mL 2.7139 mL

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纯度 & 产品资料

纯度: 98.01%

Data Sheet (613 KB) SDS (393 KB)

COA (199 KB) HNMR (158 KB) RP-HPLC (152 KB) MS (71 KB)

产品使用指南 (1538 KB)

参考文献

  • [1]. Bhat S A, et al. Angiotensin receptor blockade modulates NFκB and STAT3 signaling and inhibits glial activation and neuroinflammation better than angiotensin-converting enzyme inhibition [J]. Molecular neurobiology, 2016, 53: 6950-6967.  [Content Brief]

    [2]. Wei X, et al. Combination of perindopril erbumine and huangqi-danshen decoction protects against chronic kidney disease via sirtuin3/mitochondrial dynamics pathway [J]. Evidence-Based Complementary and Alternative Medicine, 2022, 2022.  [Content Brief]

    [3]. Afonso T, et al. Pharmacodynamic evaluation of 4 angiotensin‐converting enzyme inhibitors in healthy adult horses [J]. Journal of veterinary internal medicine, 2013, 27(5): 1185-1192.  [Content Brief]

    [4]. Thybo N K, et al. Dose-dependent effects of perindopril on blood pressure and small-artery structure [J]. Hypertension, 1994, 23(5): 659-666.  [Content Brief]

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