Perindopril Erbumine

製品コードS1506 バッチS150602

化学情報

	Synonyms	S9490-3	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₉H₃₂N₂O₅.C₄H₁₁N
	分子量	441.6	CAS No.	107133-36-8
Solubility (25°C)*	体外	Water	88 mg/mL (199.27 mM)
		Ethanol	88 mg/mL (199.27 mM)
		DMSO	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

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生物活性

製品説明	Perindopril Erbumine (S9490-3) is a pro-drug and metabolized in vivo by hydrolysis of the ester group to form Perindoprilat, the biologically active metabolite, a potent ACE inhibitor with IC50 of 1.05 nM. Perindopril Erbumine is used for in vivo studies and Perindoprilat is recommened for in vitro research.
in vitro	Perindopril Erbumine displays a higher binding affinity for the bradykinin binding sites than the angiotensin I binding sites of the angiotensin-converting enzyme (ACE) with bradykinin/angiotensin I selectivity ratio of 1.44. ^[1] Perindopril Erbumine inhibits the angiotensin- and Aβ42-to-Aβ40-converting activity of mutated ACE containing two active domains (F-ACE) with IC50 of 0.03-0.1 μM, and 0.01-0.03 μM, respectively. ^[2] Perindopril Erbumine (~2 μM) displays no significant cytotoxicity towards SCC-VII and KB cells, but can significantly reduce the production of angiotensin II and the transcription of VEGF in KB cells in a concentration-dependent manner. ^[3]
in vivo	Oral administration of Perindopril Erbumine at 2 mg/kg/day has a significant inhibitory effect on SCC-VII tumor growth, and reduces blood vessel formation surrounding the tumors in vivo due to the suppression of VEGF-induced angiogenesis. ^[3] Administration of Perindopril Erbumine at 2 mg/kg/day displays a strong inhibitory effect of the BNL-HCC tumor growth in rats similar to that of 20 mg/kg/day and in contrast to the AT1-R antagonist candesartan or losartan which at the dose of 20 mg/kg/day has no inhibitory effect. ^[4] Administration of Perindopril Erbumine at 3 mg/kg/day significantly inhibits LPS-induced apoptosis by 6.4% in RAECs in vivo than that of ramipril by 3.2%. ^[5] Administration of Perindopril Erbumine (1 mg/kg/day) significantly suppresses the hippocampal ACE activity, and prevents cognitive impairment and brain injury in rats with Alzheimer's disease (AD). ^[6]

プロトコル(参考用のみ)

キナーゼアッセイ	ACE inhibitor binding assay
キナーゼアッセイ	The binding assay is based on the competitive displacement of [¹²⁵I]351A by Perindopril Erbumine and performed on whole endothelial cells. Subconfluent HUVECs in 6-well plates are rinsed with 2 mL binding buffer (140 mM NaCl, 2.7 mM KCl, 1.8 mM CaCl₂, 1.03 mM MgCl₂, 0.42 mM NaH₂PO₄, 10 mM HEPES, 2 mM sodium pyruvate, 5 mM glucose, pH 7.4), and the culture medium is replaced with 2.5 mL fresh binding buffer containing 5% fetal bovine serum (FBS). A set concentration of Perindopril Erbumine (2.5-12.5 μL, 0.1-50 nM) is added to the binding buffer. A saturating amount of [¹²⁵I]351A (10 μL, typically 10⁶ cpm) is then added to each sample and the plates are incubated at 37 °C for 2 hours in a thermostatic bath. The cells are then rinsed twice with 1.5 mL binding buffer. Finally, the cells are extracted with 0.5 mL NaOH 1 N, incubated for 5 minutes, and the radioactivity is counted with a gamma counter. The radioactivity, which is due to [¹²⁵I]351A binding, is inversely related to Perindopril Erbumine's affinity for endothelial ACE. The concentration of Perindopril Erbumine that displaces 50% of the bound radioligand is calculated from the competition curve.
動物実験	動物モデル	Female BALB/c nude mice injected with SCC-VII cells
	投薬量	1 or 2 mg/kg/day
	投与方法	Orally

参考

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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Brain Renin-Angiotensin System Blockade Attenuates Methamphetamine-Induced Hyperlocomotion and Neurotoxicity [ Neurotherapeutics, 2018, 15(2):500-510]	PubMed: 29464572

Brain Renin-Angiotensin System Blockade Attenuates Methamphetamine-Induced Hyperlocomotion and Neurotoxicity [ Neurotherapeutics, 2018, 15(2):500-510]

PubMed: 29464572

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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