Home Transmembrane Transporters Calcium Channel inhibitor Nilvadipine For research use only.

Nilvadipine

Synonyms: ARC029, FR34235,FK235

Nilvadipine (ARC029, FR34235,FK235) is a potent calcium channel blocker with an IC50 of 0.03 nM.

Nilvadipine Chemical Structure

Nilvadipine Chemical Structure

CAS: 75530-68-6

Selleck's Nilvadipine has been cited by 10 publications

Purity & Quality Control

Batch: S272101 DMSO] 77 mg/mL] false] Ethanol] 33 mg/mL] false] Water] Insoluble] false Purity: 99.99%
99.99

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Biological Activity

Description Nilvadipine (ARC029, FR34235,FK235) is a potent calcium channel blocker with an IC50 of 0.03 nM.
Targets
Calcium channel [1]
0.03 nM
In vitro
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
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]

Chemical lnformation & Solubility

Molecular Weight 385.37 Formula

C19H19N3O6
CAS No. 75530-68-6 SDF Download Nilvadipine SDF
Smiles CC1=C(C(C(=C(N1)C#N)C(=O)OC)C2=CC(=CC=C2)[N+](=O)[O-])C(=O)OC(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 77 mg/mL ( (199.8 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 33 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

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.

Handling Instructions

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