Catalog No.S2721 Synonyms: ARC029, FR34235
Molecular Weight(MW): 385.37
Nilvadipine is a potent calcium channel blocker with an IC50 of 0.03 nM.
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4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.
|Description||Nilvadipine is a potent calcium channel blocker with an IC50 of 0.03 nM.|
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).  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. 
|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.  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.  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). |
-  Nomoto A, et al. Atherosclerosis, 1988, 72(2-3), 213-219.
-  Ozawa Y, et al. J Cardiovasc Pharmacol, 1999, 33(2), 243-247.
-  Yamazaki H, et al. Invest Ophthalmol Vis Sci, 2002, 43(4), 919-926.
|In vitro||DMSO||77 mg/mL (199.8 mM)|
|Ethanol||33 mg/mL (85.63 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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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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