Amlodipine

Catalog No.S1905 Synonyms: UK-48340

Amlodipine  Chemical Structure

Molecular Weight(MW): 408.88

Amlodipine is a long-acting calcium channel blocker, used to lower blood pressure and prevent chest pain.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 970 In stock
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Biological Activity

Description Amlodipine 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

Solubility (25°C)

In vitro DMSO 82 mg/mL (200.54 mM)
Ethanol 82 mg/mL (200.54 mM)
Water 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.

Chemical Information

Molecular Weight 408.88
Formula

C20H25ClN2O5

CAS No. 88150-42-9
Storage powder
Synonyms UK-48340

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02995720 Active, not recruiting Hypertension, Hyperlipidemia Boryung Pharmaceutical Co., Ltd August 26, 2016 Phase 1
NCT02699645 Not yet recruiting Acute Intracerebral Haemorrhage (ICH) The George Institute May 2017 Phase 4
NCT02969265 Not yet recruiting Hypertension Takeda May 2017 Phase 3
NCT02940548 Recruiting Hypertension Jing Liu|Bayer|Peking University Peoples Hospital December 2016 Phase 4
NCT02988362 Not yet recruiting Hypertension HanAll BioPharma Co., Ltd. December 2016 Phase 1
NCT02973035 Recruiting Hypertension Asan Medical Center|Yuhan Corporation December 2016 Phase 4

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID