2. Membrane Transporter/Ion Channel
  3. Chloride Channel
  4. Emidurdar

Emidurdar  (Synonyms: Endovion; NS3728)

Cat. No.: HY-105917 Purity: 99.13%
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Endovion (NS3728) est un inhibiteur du canal anionique (comme le canal chlorure) pharmacologique et le bloqueur spécifique du VRAC/VSOAC. Endovion (NS3728) est également un inhibiteur du canal Anoctamin-1 (ANO 1).

Endovion is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.

For research use only. We do not sell to patients.

Emidurdar Chemical Structure

Emidurdar Chemical Structure

CAS No. : 265646-85-3

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Based on 4 publication(s) in Google Scholar

Emidurdar Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

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Description

Endovion is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor[1][2].

IC50 & Target

Chloride channel, VRAC/VSOAC[1].
ANO1[2].
In Vitro

Endovion (NS3728, 10-100 μM) reduces TNFα-induced apoptosis and increases p53-protein level as well as downstream signaling, e.g., expression of p21Waf1/Cip1, Bax, Noxa, MDM2, and activation of Caspase-9/-3 in Cisplatin-sensitive cells[1].
Endovion (NS3728, 10 μM) inhibits cell proliferation in Capan-1, AsPC-1 and BxPC-3 cell lines[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Emidurdar Related Antibodies

Western Blot Analysis[1]

Cell Line: Wild-type, resistant, and transiently transfected A2780 cells.
Concentration: 10-100 μM.
Incubation Time: 18 or 4.5 h.
Result: Reduced the maximal taurine rate constant more than 90% compared with the untreated control cells.
Resulted in an increased LRRC8A protein expression.
Significantly reduceed p53 and p21Waf1/Cip1 protein level in A2780WT cells.

Cell Proliferation Assay[2]

Cell Line: Capan-1, AsPC-1, BxPC-3 and H6c7 cell lines.
Concentration: 10 μM.
Incubation Time: 24 h.
Result: Resulted in the most pronounced inhibition in all cell lines with 77 ± 26 % in Capan-1, 67 ± 9 % in AsPC-1, and 54 ± 8 % in BxPC-3 cells at +67 mV.
Molecular Weight

495.18

Formula

C16H9BrF6N6O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)C1=CC(C(F)(F)F)=CC(NC(NC2=C(C3=NN=NN3)C=C(Br)C=C2)=O)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (252.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0195 mL 10.0973 mL 20.1947 mL
5 mM 0.4039 mL 2.0195 mL 4.0389 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0195 mL 10.0973 mL 20.1947 mL 50.4867 mL
5 mM 0.4039 mL 2.0195 mL 4.0389 mL 10.0973 mL
10 mM 0.2019 mL 1.0097 mL 2.0195 mL 5.0487 mL
15 mM 0.1346 mL 0.6732 mL 1.3463 mL 3.3658 mL
20 mM 0.1010 mL 0.5049 mL 1.0097 mL 2.5243 mL
25 mM 0.0808 mL 0.4039 mL 0.8078 mL 2.0195 mL
30 mM 0.0673 mL 0.3366 mL 0.6732 mL 1.6829 mL
40 mM 0.0505 mL 0.2524 mL 0.5049 mL 1.2622 mL
50 mM 0.0404 mL 0.2019 mL 0.4039 mL 1.0097 mL
60 mM 0.0337 mL 0.1683 mL 0.3366 mL 0.8414 mL
80 mM 0.0252 mL 0.1262 mL 0.2524 mL 0.6311 mL
100 mM 0.0202 mL 0.1010 mL 0.2019 mL 0.5049 mL
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Emidurdar Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Emidurdar265646-85-3Endovion NS3728NS3728NS 3728NS-3728Chloride ChannelCl− ChannelsInhibitorinhibitorinhibit

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