1. Membrane Transporter/Ion Channel
  2. Chloride Channel
  3. Endovion

Endovion (Synonyms: NS3728)

Cat. No.: HY-105917 Purity: 99.27%
Handling Instructions

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 (NS3728) 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.

Endovion Chemical Structure

Endovion Chemical Structure

CAS No. : 265646-85-3

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10 mM * 1 mL in DMSO USD 99 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Endovion (NS3728) 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].

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

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.

265646-85-3

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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (252.43 mM; Need ultrasonic)

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
10 mM 0.2019 mL 1.0097 mL 2.0195 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

EndovionNS3728NS 3728NS-3728Chloride ChannelCl− ChannelsInhibitorinhibitorinhibit

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