Nilvadipine

Catalog No.S2721

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

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Nilvadipine Chemical Structure

Nilvadipine Chemical Structure
Molecular Weight: 385.37

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Nilvadipine is available in the following compound libraries:

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Product Description

Biological Activity

Description Nilvadipine is a potent calcium channel blocker with an IC50 of 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]
Features

Protocol(Only for Reference)

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Nomoto A, et al. Atherosclerosis, 1988, 72(2-3), 213-219.

[2] Ozawa Y, et al. J Cardiovasc Pharmacol, 1999, 33(2), 243-247.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-09-20)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02017340 Recruiting Alzheimers Disease Prof Brian Lawlor|University of Dublin, Trinity College|M  ...more 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

Chemical Information

Download Nilvadipine SDF
Molecular Weight (MW) 385.37
Formula

C19H19N3O6

CAS No. 75530-68-6
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms ARC029, FR34235
Solubility (25°C) * In vitro DMSO 77 mg/mL (199 mM)
Water <1 mg/mL (<1 mM)
Ethanol 33 mg/mL (85 mM)
* <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.
Chemical Name 5-isopropyl 3-methyl 2-cyano-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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