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Ethaverine hydrochloride

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Catalog No. T0369Cas No. 985-13-7
Alias Papetherine, Ethaquin, Consenil

Ethaverine hydrochloride is a homologue of papaverine and is used as a vasodilator and antispasmodic.[2]

Ethaverine hydrochloride

Ethaverine hydrochloride

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🥰Excellent
Purity: 99.90%
Catalog No. T0369Alias Papetherine, Ethaquin, ConsenilCas No. 985-13-7
Ethaverine hydrochloride is a homologue of papaverine and is used as a vasodilator and antispasmodic.[2]
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$37In StockIn Stock
5 mg$57In StockIn Stock
10 mg$103In StockIn Stock
25 mg$177In StockIn Stock
50 mg$263In StockIn Stock
100 mg$377In StockIn Stock
1 mL x 10 mM (in DMSO)$78In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.90%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Ethaverine hydrochloride AI Summary
Ethaverine hydrochloride exhibits a diverse range of bioactivities, demonstrating potency in several biological assays. It functions as an enhancer of SMN2 splice variant expression and inhibits multiple targets, including ROR gamma transcriptional activity, the ERK signaling pathway, 15-human lipoxygenase 2, Polymerase Kappa, USP1/UAF1, human tyrosyl-DNA phosphodiesterase 1 (TDP1), as well as both Vaccinia Orthopoxvirus and Marburg Virus entry into cells. Additionally, this compound effectively blocks Ebola Virus entry. Specifically, Ethaverine hydrochloride inhibits sodium fluorescein uptake in both OATP1B3-transfected CHO cells and OATP1B1-transfected CHO cells at a concentration of 10 µM, with respective inhibition percentages of 156.16% and 524.92%. It also exhibits moderate activity in reducing the viability of SARS-CoV-2 infected Vero E6 cells, with an inhibition index of 0.4908. Moreover, the compound shows strong antiviral activity against SARS-CoV-2, evidenced by a 99.42% inhibition of virus-induced cytotoxicity in Caco-2 cells at 10 µM after 48 hours and a low IC50 value of 640.0 nM. It has a selectivity index of 17.0, suggesting a favorable therapeutic profile. However, it shows 11.3% inhibition of the SARS-CoV-2 3CL-Pro protease at 20 µM. Despite this, the assay results for VERO-6 cells indicated an inhibition percentage of -0.08% under the tested conditions. Overall, Ethaverine hydrochloride is a multifaceted agent with significant potential across various biological and antiviral applications..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Ethaverine hydrochloride is a homologue of papaverine and is used as a vasodilator and antispasmodic.[2]
In vitro
METHODS: The inhibitory effect of ethaverine on dopamine content in PC12 cells was studied.
RESULTS Ethaverine reduced dopamine content in PC12 cells in a concentration-dependent manner. At a concentration of 1.0 μM, dopamine content was inhibited by 33.6% within 24-48 hours. The IC50 value of ethaverine was 1.4 μM. 2.0 μM ethaverine reduced dopamine content after 6 hours of action. Tyrosine hydroxylase (TH) was inhibited after 6 hours of ethaverine treatment in PC12 cells, and the activity remained at a reduced level until 36 hours (the inhibition rate was 12-22% at 2.0 μM). [1]
Ethaverine (10 μM) treatment in PC12 cells reduces catecholamine secretion by blocking L-type voltage-sensitive Ca2+ channels. [2]
In vivo
METHODS: In a short-term experiment on 11 guinea pigs, the effect of Ethaverine hydrochloride on cochlear microcirculation was observed (2/5 and /10 mg/kg, i.v) for 10 minutes. In these experiments, intracochlear PO2, intracochlear potential (EP), cochlear microphonic (CM) potential, and blood pressure (BP) were recorded. Intracochlear PO2 was measured polarographically in the mid-level using gold electrodes.
RESULTS Ethaverine hydrochloride at doses of 5 and 10 mg/kg caused a significant increase in intracochlear PO2 for 35 to 90 minutes, even with a temporary decrease in blood pressure. At the same time, this improvement in cochlear microcirculation was observed to coincide with an increase in CM potential. The decrease in EP may be the result of a decrease in blood pressure and a direct effect of Ethaverine hydrochloride on EP production. [3]
SynonymsPapetherine, Ethaquin, Consenil
Chemical Properties
Molecular Weight431.96
FormulaC24H30ClNO4
Cas No.985-13-7
SmilesCCOc1c(OCC)cc(Cc2nccc3cc(OCC)c(OCC)cc23)cc1.Cl
Relative Density.1.104g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
H2O: 100 mg/mL (231.5 mM), Sonication is recommended.
DMSO: 16 mg/mL (37.04 mM), Sonication is recommended.
Solution Preparation Table
DMSO/H2O
1mg5mg10mg50mg
1 mM2.3150 mL11.5751 mL23.1503 mL115.7515 mL
5 mM0.4630 mL2.3150 mL4.6301 mL23.1503 mL
10 mM0.2315 mL1.1575 mL2.3150 mL11.5751 mL
20 mM0.1158 mL0.5788 mL1.1575 mL5.7876 mL
H2O
1mg5mg10mg50mg
50 mM0.0463 mL0.2315 mL0.4630 mL2.3150 mL
100 mM0.0232 mL0.1158 mL0.2315 mL1.1575 mL

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Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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