Amlodipine

製品コードS1905 バッチS190501

化学情報

	Synonyms	UK-48340	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₀H₂₅ClN₂O₅
	分子量	408.88	CAS No.	88150-42-9
Solubility (25°C)*	体外	DMSO	82 mg/mL (200.54 mM)
		Ethanol	82 mg/mL (200.54 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.

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生物活性

製品説明	Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
in vitro	Amlodipine causes a dose-dependent increase in nitrite production. Amlodipine also increases nitrite production in large coronary arteries and in aorta. ^[1] Amlodipine is attributed to distinct membrane physico-chemical interactions. Amlodipine contributes to distinct membrane biophysical interactions that lead to potent lipid antioxidant effects, independent of calcium channel modulation. ^[2] Amlodipine increases plaque smooth muscle cell content (P<0.05), whereas atenolol decreases plaque inflammation. ^[3] Amlodipine attenuates intracellular neuronal Ca²⁺ increases elicited by KCl depolarization but does not affect Ca²⁺ changes triggered by N-methyl-D-aspartate receptor activation. Amlodipine also inhibits free radical-induced damage to lipid constituents of the membrane in a dose-dependent manner, independent of Ca²⁺ channel modulation. ^[4]
in vivo	Amlodipine results in regression of cardiovascular hypertrophy and amelioration of endothelial dysfunction in spontaneously hypertensive rats. ^[5] Amlodipine significantly reduces aortic hypertrophy, endothelial dysfunction, LOX-1 expression, aortic O(2)(-) and ONOO(-) production, and plasma free 8-F(2)alpha-isoprostane levels in Ang II-infused rats. Amlodipine has antihypertensive and antioxidant activity in vivo, which effectively inhibits many of the oxidative stress-dependent mechanisms involved in Ang II-mediated cardiovascular injury. ^[6]

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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：

KCTD4 interacts with CLIC1 to disrupt calcium homeostasis and promote metastasis in esophageal cancer [ Acta Pharm Sin B, 2023, 13(10):4217-4233]	PubMed: 37799381
Anticancer Effects of Amlodipine Alone or in Combination With Gefitinib in Non-Small Cell Lung Cancer [ Front Pharmacol, 2022, 13:902305]	PubMed: 35721193
Repurposing screen identifies Amlodipine as an inducer of PD-L1 degradation and antitumor immunity [ Oncogene, 2021, 40(6):1128-1146]	PubMed: 33323966
High-Throughput Screening of an FDA-Approved Drug Library Identifies Inhibitors against Arenaviruses and SARS-CoV-2 [ ACS Infect Dis, 2020, acsinfecdis.0c00486]	PubMed: 33183004
Development and Feasibility of a Porcine Model of Amlodipine Toxicity. [ J Med Toxicol, 2020, 16(1):61-66]	PubMed: 31385194
Induction of store-operated calcium entry (SOCE) suppresses glioblastoma growth by inhibiting the Hippo pathway transcriptional coactivators YAP/TAZ. [ Oncogene, 2019, 38(1):120-139]	PubMed: 30082911
Selective uveal melanoma inhibition with calcium channel blockade. [ Int J Oncol, 2019, 55(5):1090-1096]	PubMed: 31545410
Evaluation system for arrhythmogenic potential of drugs using human-induced pluripotent stem cell-derived cardiomyocytes and gene expression analysis [Higa A, et al. J Toxicol Sci, 2017, 42(6):755-761]	PubMed: 29142174

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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