Lercanidipine hydrochloride

製品コードS4597 バッチS459702

化学情報

	Synonyms		Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₃₆H₄₁N₃O₆.HCl
	分子量	648.19	CAS No.	132866-11-6
Solubility (25°C)*	体外	DMSO	66 mg/mL (101.82 mM)
		Ethanol	1 mg/mL (1.54 mM)
		Water	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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Lercanidipine is a calcium channel blocker of the dihydropyridine class.
in vitro	In vitro calcium antagonistic activity of Lercanidipine is clearly related to a gradual block of calcium entry into smooth muscle cells via L-type calcium channels. lercanidipine inhibits cellular cholesteryl ester formation. At concentrations similar to those occurring in clinical practice, it may inhibit in vitro macrophage functions involved in atherogenesis and plaque stability^[1].
in vivo	In chronically catheterised dogs with experimental renovascular hypertension, lercanidipine decreases diastolic blood pressure in a dose-dependent manner (ED25 = 0.9 mg/kg p.o). In the same animals, long term application of lercanidipine showed permanent decrease of diastolic blood pressure indicating no tolerance of the antihypertensive effect^[3]. Lercanidipine possesses significant anticonvulsant effect. It does not affect the muscle coordination or locomotor activity in mice^[5]. In clinical studies, lercanidipine has a 24-hour antihypertensive effect and causes no significant increase in heart rate. Lercanidipine has been shown to be effective in a wide range of hypertensive patients, including mild-to-moderate hypertension, severe hypertension, the elderly, and those with isolated systolic hypertension. It is associated with a low rate of adverse events^[4].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Mouse peritoneal macrophages
	濃度	0.1, 1, 5, 10, 15 μM
	反応時間	48 h
	実験の流れ	Cells are incubated for 24 hours in DMEM+EFAF 0.2% and lercanidipine, then with lercanidipine and AcLDL for 24 hours. In the last 2 hours [14C]-oleic acid albumin complex is added for the determination of cholesterol esterification (ACAT activity).
動物実験	動物モデル	Adult male Swiss albino mice
	投薬量	1 and 3 mg/kg
	投与方法	i.p.

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：

Structure-dependent complexation of Fe3+ by anthracyclines. 2. The roles of methoxy and daunosamine functionalities [Nawara K, et al. J Phys Chem B, 2013, 117(23):6868-73]	PubMed: 23692121

Structure-dependent complexation of Fe3+ by anthracyclines. 2. The roles of methoxy and daunosamine functionalities [Nawara K, et al. J Phys Chem B, 2013, 117(23):6868-73]

PubMed: 23692121

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。