Efonidipine

For research use only.

Catalog No.S4977 Synonyms: NZ-105

Efonidipine Chemical Structure

CAS No. 111011-63-3

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.

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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

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].

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].

Protocol

Cell Research:[2]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • 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.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (158.31 mM)
Ethanol '40 mg/mL

* 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 Information

Molecular Weight 631.66
Formula

C34H38N3O7P

CAS No. 111011-63-3
Storage powder
in solvent
Synonyms NZ-105
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID