Amlodipine

Catalog No.S1905 Batch:S190503

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Technical Data

Formula

C20H25ClN2O5

Molecular Weight 408.88 CAS No. 88150-42-9
Solubility (25°C)* In vitro 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Amlodipine (UK-48340) is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.
Targets
Calcium channel [1]
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]

Protocol (from reference)

Selleck's Amlodipine has been cited by 8 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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