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

Efonidipine

Synonyms: NZ-105

Efonidipine (NZ-105) is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. It also suppresses aldosterone secretion from the adrenal.

Efonidipine Chemical Structure

Efonidipine Chemical Structure

CAS No. 111011-63-3

Purity & Quality Control

Efonidipine Related Products

Signaling Pathway

Calcium Channel Signaling Pathways

Calcium Channel Signaling Pathway

Biological Activity

Description Efonidipine (NZ-105) is an L- and T-type calcium channel blocker leading to vasodilation and decreased automaticity of the heart. It also suppresses aldosterone secretion from the adrenal.
Targets
T-type calcium channel [2]
In vitro
In vitro Although efonidipine is not a specific T-type calcium channe (TTCC) blocker as it could also block L-type calcium channe (LTCC), its efficacy in blocking TTCC is much greater than that of LTCC[1]. Efonidipine exerts an inhibitory effect on aldosterone synthesis and secretion in a human adrenocortical cell line (H295R), an effect that is mediated, at least in part, by suppression of 11-β-hydroxylase and aldosterone synthase expression. Efonidipine also suppresses both Ang II- and K+-induced aldosterone secretion, but it blocks the latter at much lower concentrations than the former[2].
Cell Research Cell lines The NCI-H295R human adrenocortical cell line (H295)
Concentrations 0.3 μM and 3 μM
Incubation Time 24 h
Method H295R cells are plated to a density of 0.2 × 106 in 6-well plates and incubated for 48 hours, after which the medium is replaced with low-serum medium containing 0.2% UltroserSF, and the cells are then treated with Ang II (100 nmol/L) or KCl (10 mmol/L) with or without the indicated concentration of Ca2+ channel blocker for 24 hours. The cells are then harvested, and the total cellular RNA is extracted using the isothiocyanate-acid phenol chloroform method. After quantifying the extracted RNA based on absorbance at 260 nm, 500-ng aliquots are reverse transcribed.
In Vivo
In vivo Efonidipine could provide broader beneficial effects including the heart, liver, and plasma, and antioxidant in iron-overload condition in both WT(muβ+⁄+) and HT(muβth-3 ⁄+,) mice[1].
Animal Research Animal Models adult C57/BL6 mice (3-6 months old, heterozygous βKO type) with FE diet (0.2% ferrocene w⁄w)
Dosages 4 mg⁄kg
Administration i.p.

Chemical Information & Solubility

Molecular Weight 631.66 Formula

C34H38N3O7P
CAS No. 111011-63-3 SDF --
Smiles CC1=C(C(C(=C(N1)C)P2(=O)OCC(CO2)(C)C)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OCCN(CC4=CC=CC=C4)C5=CC=CC=C5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (158.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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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.

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