A dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC50 = 0.148 µM); activates TRPA1 channels

Nicardipine (hydrochloride) – 1 g

Brand:
Cayman
CAS:
54527-84-3
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

Nicardipine is a dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity.{28535} It is reported to inhibit adenosine A1, A2A, and A3 receptors with Ki values of 19.6, 63.8, and 3.25 µM, respectively, and can inhibit cytochrome P450 3A4 catalytic activity with an IC50 value of 0.148 µM.{28536,27561} Additionally, nicardipine has been shown to activate transient receptor potential A1 channels, producing an increase in Ca2+ (EC50 = 0.5 µM).{23938}  

 

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Description

A dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC50 = 0.148 µM); activates TRPA1 channels, producing an increase in Ca2+ (EC50 = 0.5 µM)

Formal name: 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid, 3-methyl 5-[2-[methyl(phenylmethyl)amino]ethyl] ester, monohydrochloride

Synonyms:  RS 69216

Molecular weight: 516

CAS: 54527-84-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|Cytochrome P450||Research Area|Cardiovascular System|Cardiovascular Diseases|Angina||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cell Biology|Cell Signaling|Calcium Mobilization

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