For research use only. Not for therapeutic Use.
Nilvadipine (Cat No.:I004795) is a highly potent calcium channel blocker that effectively inhibits the influx of calcium ions into cells. It acts by specifically targeting and blocking the L-type calcium channels in smooth muscle cells, resulting in vasodilation and decreased vascular resistance. This mechanism of action makes Nilvadipine useful in the treatment of hypertension and certain cardiovascular conditions. With an IC50 value of 0.03 nM, it demonstrates strong affinity and efficacy in blocking calcium channels, contributing to its therapeutic effectiveness in regulating blood pressure and improving cardiovascular health.
| Catalog Number | I004795 |
| CAS Number | 75530-68-6 |
| Synonyms | 3-O-methyl 5-O-propan-2-yl 2-cyano-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| Molecular Formula | C19H19N3O6 |
| Purity | ≥95% |
| Target | Neuronal Signaling |
| Solubility | DMSO 77 mg/mL; Water <1 mg/mL |
| Storage | 2-8°C |
| IUPAC Name | 3-O-methyl 5-O-propan-2-yl 2-cyano-6-methyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate |
| InChI | InChI=1S/C19H19N3O6/c1-10(2)28-19(24)15-11(3)21-14(9-20)17(18(23)27-4)16(15)12-6-5-7-13(8-12)22(25)26/h5-8,10,16,21H,1-4H3 |
| InChIKey | FAIIFDPAEUKBEP-UHFFFAOYSA-N |
| SMILES | CC1=C(C(C(=C(N1)C#N)C(=O)OC)C2=CC(=CC=C2)[N+](=O)[O-])C(=O)OC(C)C |
| Reference | </br>1:European multicentre double-blind placebo-controlled trial of Nilvadipine in mild-to-moderate Alzheimer/’s disease-the substudy protocols: NILVAD frailty; NILVAD blood and genetic biomarkers; NILVAD cerebrospinal fluid biomarkers; NILVAD cerebral blood flow. Meulenbroek O, O/’Dwyer S, de Jong D, van Spijker G, Kennelly S, Cregg F, Olde Rikkert M, Abdullah L, Wallin A, Walsh C, Coen R, Kenny RA, Daly L, Segurado R, Borjesson-Hanson A, Crawford F, Mullan M, Lucca U, Banzi R, Pasquier F, Breuilh L, Riepe M, Kalman J, Molloy W, Tsolaki M, Howard R, Adams J, Gaynor S, Lawlor B.BMJ Open. 2016 Jul 19;6(7):e011584. doi: 10.1136/bmjopen-2016-011584. PMID: 27436668 Free PMC Article</br>2:Correction. NILVAD protocol: a European multicenter double-blind placebo-controlled trial of nilvadipine in mild-to-moderate Alzheimer/’s disease. Lawlor B, Kennelly S, O/’Dwyer S.BMJ Open. 2015 Sep 28;5(9):e006364. doi: 10.1136/bmjopen-2014-006364corr1. No abstract available. PMID: 26416510 Free PMC Article</br>3:NILVAD protocol: a European multicentre double-blind placebo-controlled trial of nilvadipine in mild-to-moderate Alzheimer/’s disease. Lawlor B, Kennelly S, O/’Dwyer S, Cregg F, Walsh C, Coen R, Kenny RA, Howard R, Murphy C, Adams J, Daly L, Segurado R, Gaynor S, Crawford F, Mullan M, Lucca U, Banzi R, Pasquier F, Breuilh L, Riepe M, Kalman J, Wallin A, Borjesson A, Molloy W, Tsolaki M, Olde Rikkert M.BMJ Open. 2014 Oct 9;4(10):e006364. doi: 10.1136/bmjopen-2014-006364. Erratum in: BMJ Open. 2015;5(9):e006364. PMID: 25300460 Free PMC Article</br>4:Histological protection by nilvadipine against neurotoxicity induced by NOC12, a nitric oxide donor, in the rat retina. Kuroki T, Mori A, Nakahara T, Sakamoto K, Ishii K.Biol Pharm Bull. 2014;37(2):306-10. PMID: 24492726 Free Article</br>5:Long-term effects of nilvadipine against progression of the central visual field defect in retinitis pigmentosa: an extended study. Nakazawa M, Suzuki Y, Ito T, Metoki T, Kudo T, Ohguro H.Biomed Res Int. 2013;2013:585729. doi: 10.1155/2013/585729. Epub 2013 Nov 12. PMID: 24319686 Free PMC Article</br>6:Factors affecting the absorption of nilvadipine from disintegration-controlled matrix tablet in dogs. Sakai T, Sako K, Hayashi M.Biol Pharm Bull. 2011;34(11):1731-6. PMID: 22040887 Free Article</br>7:Demonstration of safety in Alzheimer/’s patients for intervention with an anti-hypertensive drug Nilvadipine: results from a 6-week open label study. Kennelly SP, Abdullah L, Paris D, Parish J, Mathura V, Mullan M, Crawford F, Lawlor BA, Kenny RA.Int J Geriatr Psychiatry. 2011 Oct;26(10):1038-45. doi: 10.1002/gps.2638. Epub 2010 Oct 29. PMID: 21905098 </br>8:Apolipoprotein E genotype-specific short-term cognitive benefits of treatment with the antihypertensive nilvadipine in Alzheimer/’s patients–an open-label trial. Kennelly S, Abdullah L, Kenny RA, Mathura V, Luis CA, Mouzon B, Crawford F, Mullan M, Lawlor B.Int J Geriatr Psychiatry. 2012 Apr;27(4):415-22. doi: 10.1002/gps.2735. Epub 2011 May 10. PMID: 21560164 </br>9:Calcium channel blocker nilvadipine, but not diltiazem, inhibits ocular inflammation in endotoxin-induced uveitis. Ishida S, Koto T, Nagai N, Oike Y.Jpn J Ophthalmol. 2010 Nov;54(6):594-601. doi: 10.1007/s10384-010-0862-5. Epub 2010 Dec 30. PMID: 21191722 </br>10:Effect of nilvadipine on central visual field in retinitis pigmentosa: a 30-month clinical trial. Nakazawa M, Ohguro H, Takeuchi K, Miyagawa Y, Ito T, Metoki T.Ophthalmologica. 2011;225(2):120-6. doi: 10.1159/000320500. Epub 2010 Oct 16. PMID: 20948238 |
