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Econazole nitrate Calcium Channel modulator

Name: Econazole nitrate
Brand: Selleck Chemicals
SKU: S2535
Availability: InStock
Rating: 5 (4 reviews)

Cat.No.S2535

Econazole Nitrate (NSC 243115,Spectazole) is a Ca2+ channel blocker, used as an antifungal medicine that fights infections caused by fungus.

Chemical Structure

Molecular Weight: 444.7

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.22%

99.22

Related Targets	CD markers AChR Sodium Channel Potassium Channel GABA Receptor ATPase TRP Channel GluR NMDAR P2 Receptor Proton Pump P-gp CFTR SGLT Chloride Channel MCT Amino acid transporter GLUT CRM1 VDAC BCRP NKCC OCT NCX OAT VMAT Aquaporin EAAT GlyT GlyR
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Chemical Information, Storage & Stability

Molecular Weight	444.7	Formula	C₁₈H₁₅Cl₃N₂O.HNO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	24169-02-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC 243115,Spectazole			Smiles	C1=CC(=CC=C1COC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl)Cl.[N+](=O)(O)[O-]

Solubility

In vitro
Batch:

DMSO : 89 mg/mL ( (200.13 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	Calcium channel ^[1]
In vitro	Econazole nitrate is an effective inducer of micronuclei over a narrow dose range in cell lines V79, XEM2 and XEMd-MZ (expresses CYP1A2). ^[1] This compound inhibits the proliferation of MCF-7 cells in a time- and dose-dependent manner by MTT method and colony forming assay. This compound results in typical characteristics of apoptosis including the morphological changes and DNA fragmentation in MCF-7 cells. This compound results in the decrease expression of procaspase-3, procaspase-9 and bcl-2. ^[2] This compound inhibits ADP-ribose-activated currents in HEK-293 cells expressing recombinant human TRPM2 (hTRPM2). This compound produces an essentially complete inhibition of the TRPM2-mediated current. ^[3] This compound (25-50 mM) partially inhibits capacitative Ca2+ entry induced by cyclopiazonic acid, another endoplasmic reticulum Ca2+ pump inhibitor. This compound induces Ca2+ influx via two separate pathways: one is sensitive to La3+, the other is not. ^[4] This compound reversibly inhibits (Bu)(2)cAMP-stimulated progesterone production in a dose- and time-dependent manner in MA-10 cells without affecting total protein synthesis or P450(scc) and 3beta-hydroxysteroid dehydrogenase (3beta-HSD) enzyme expression or activity. ^[5] This compound is a store-operated Ca2+ channel antagonist which induces cytotoxic cell death of leukemia. This compound (5-20 mM) arrests human colon cancer cells at the G0/G1 phase of the cell cycle. This compound induces COLO 205 cells apoptosis evidenced by ladder formation in DNA fragmentation assay and sub-G1 peak. ^[6]
References	https://pubmed.ncbi.nlm.nih.gov/16423345/ https://pubmed.ncbi.nlm.nih.gov/25587322/ https://pubmed.ncbi.nlm.nih.gov/15549272/ https://pubmed.ncbi.nlm.nih.gov/9990306/ https://pubmed.ncbi.nlm.nih.gov/11282276/ https://pubmed.ncbi.nlm.nih.gov/15919146/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01696799	Completed	Interdigital Tinea Pedis	AmDerma\|AmDerma Pharmaceuticals LLC	September 2011	Phase 2

Tech Support

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