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: 111011-63-3

Selleck's Efonidipine has been cited by 1 publication

Purity & Quality Control

Batch: Purity: 99.05%
99.05

Efonidipine Related Products

Signaling Pathway

Calcium Channel Signaling Pathways

Calcium Channel Signaling Pathway

Choose Selective Calcium Channel Inhibitors

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Efonidipine | Efonidipine supplier | purchase Efonidipine | Efonidipine cost | Efonidipine manufacturer | order Efonidipine | Efonidipine distributor