Nilvadipine

Catalog No.S2721 Synonyms: ARC029, FR34235

Nilvadipine Chemical Structure

Molecular Weight(MW): 385.37

Nilvadipine is a potent calcium channel blocker with an IC50 of 0.03 nM.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 270 In stock
USD 570 In stock
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Biological Activity

Description Nilvadipine is a potent calcium channel blocker with an IC50 of 0.03 nM.
Targets
Calcium channel [1]
0.03 nM
In vitro

Nilvadipine strongly inhibits the chemotaxis of interleukin-1 (IL-1), leukotriene B4 (LTB4), platelet-derived growth factor (PDGF) with IC50 of 0.1 nM in rat aortic smooth muscle cells (SMC). [1] Nilvadipine is reported to increase renal blood flow and reduce filtration fraction in the isolated perfused hydronephrotic kidney, suggesting indirectly afferent and efferent arteriolar vasodilation. [2]

In vivo Nilvadipine preserves retinal morphology and electroretinogram responses in RCS rats during the initial stage of retinal degeneration. Nilvadipine significantly enhances rhodopsin kinase and alphaA-crystallin expression and suppression of caspase 1 and 2 expression in the retina of RCS rats. [3] Nilvadipine completely inhibits the vasoactivity elicited by Abeta in rat aortae and in human middle cerebral arteries. Nilvadipine restores cortical perfusion levels in Tg APPsw to values similar to those observed in control littermates without notably affecting the CBF of control mice. [4] Nilvadipine suppresses ischemia (20 min)-reflow (20 min)-induced paw edema of mice (ED30:0.4 mg/kg i.v. and 2 mg/kg p.o.). Nilvadipine suppresses carrageenan-induced paw edema (ED30:15 mg/kg in rats and 20 mg/kg in mice) at a potency corresponding to that of an anti-inflammatory drug, ibuprofen. Nifedipine, nicardipine and nimodipine results in a suppression of 30% only with 100 mg/kg oral dosing in rats. Nilvadipine inhibits superoxide radical (O-2production from xanthine oxidase (XOD) both with lactate dehydrogenase + NADH method and cytochrome c method (IC50:90 and 100 mg/mL, respectively). [5]

Protocol

Solubility (25°C)

In vitro DMSO 77 mg/mL (199.8 mM)
Ethanol 33 mg/mL (85.63 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 385.37
Formula

C19H19N3O6

CAS No. 75530-68-6
Storage powder
Synonyms ARC029, FR34235

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02017340 Active, not recruiting Alzheimers Disease Prof Brian Lawlor|University of Dublin, Trinity College|Molecular Medicine Ireland LBG|Alzheimer Europe|Archer Pharmaceuticals, Inc.|E-Search Limited|University College Dublin|GABO:mi|Kings College London|Istituto Di Ricerche Farmacologiche Mario Negri|University Hospital, Lille|University of Ulm|Szeged University|Goeteborgs Universitet|University College Cork|Aristotle University Of Thessaloniki|Stichting Katholieke Universiteit|St. Jamess Hospital, Ireland October 2012 Phase 3

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Calcium Channel Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID