[CAS NO. 265646-85-3]  Emidurdar

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PRODUCTS SPECIFICATIONS [265646-85-3]

Catalog
HY-105917
Brand
MCE
CAS
265646-85-3

DESCRIPTION [265646-85-3]

Overview

MDL-
Molecular Weight495.18
Molecular FormulaC16H9BrF6N6O
SMILESFC(F)(F)C1=CC(C(F)(F)F)=CC(NC(NC2=C(C3=NN=NN3)C=C(Br)C=C2)=O)=C1

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

1 Publications Citing Use of MCE


Summary

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 p21 Waf1/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.

Appearance

Solid


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)

H 2 O : < 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 available by MCE.