1. Membrane Transporter/Ion Channel Apoptosis
  2. Potassium Channel Apoptosis
  3. NS-1619

NS-1619 is an opener of large conductance Ca2+-activated K+ (BK) channel. NS-1619 is a highly effective relaxant with an EC50 of about 10 – 30 μM in several smooth muscles of blood vessels and other tissues. NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells.

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NS-1619 Chemical Structure

NS-1619 Chemical Structure

CAS No. : 153587-01-0

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 132 In-stock
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Based on 2 publication(s) in Google Scholar

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Description

NS-1619 is an opener of large conductance Ca2+-activated K+ (BK) channel. NS-1619 is a highly effective relaxant with an EC50 of about 10 – 30 μM in several smooth muscles of blood vessels and other tissues[1]. NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells[2].

In Vitro

NS1619 (5, 10, 30, 50, and 100 μM) inhibits the proliferation of A2780 cells in a dosage and time dependent manner IC50=31.1 μM for 48 h pretreatment[2].
NS1619 (30 μM) exhibits augmenting effect on whole cell IK in human ovarian cancer cells A2780[2].
NS1619 (10, 30, 50, and 100 μM) increases levels of p53, p21Cip1 and Bax proteins in A2780 cells[2].
DNA content of A2780 cells was significantly decreased after 36 and 48 h of pretreatment. The breakdown of DNA results in death of the tumor cells[2].

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

Cell Viability Assay[2]

Cell Line: The human ovarian cancer cell line A2780
Concentration: 5, 10, 30, 50, and 100 μM
Incubation Time: 48 hours
Result: Inhibited cell growth in a time and concentration-dependent manner, IC50=31.1 μM.
Proliferation was significantly inhibited at concentrations of NS1619 higher than 10 μM.

Western Blot Analysis[2]

Cell Line: A2780 cells
Concentration: 0, 5, 10, 30, 50, and 100 μM
Incubation Time: 48 hours
Result: Expression of p53, p21, and Bax in A2780 cells was significantly increased in comparison with control.

Western Blot Analysis[2]

Cell Line: A2780 cells
Concentration: 30 μM
Incubation Time: 36 and 48 hours
Result: DNA content of A2780 cells was significantly decreased after 36 and 48 h of pretreatment. The breakdown of DNA results in death of the tumor cells.
In Vivo

Opening of KCa channels with NS-1619 (1 mg/kg; i.p.) can delay protection in mouse hearts[3].

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

Animal Model: Adult male outbred ICR mice[3]
Dosage: 1 mg/kg
Administration: Pretreated i.p. 24 h before I/R
Result: Pretreatment induced delayed protection 24 h later.
Resulted in significant cardioprotection 24 h later, i.e., infarct size was reduced from 38.8 ± 3.7% to 19.8 ± 2.9%.
Molecular Weight

362.23

Formula

C15H8F6N2O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=CC(C(F)(F)F)=CC=C2N1C3=CC(C(F)(F)F)=CC=C3O

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 : ≥ 31 mg/mL (85.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7607 mL 13.8034 mL 27.6068 mL
5 mM 0.5521 mL 2.7607 mL 5.5214 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.

  • Molarity Calculator

  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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 2.7607 mL 13.8034 mL 27.6068 mL 69.0169 mL
5 mM 0.5521 mL 2.7607 mL 5.5214 mL 13.8034 mL
10 mM 0.2761 mL 1.3803 mL 2.7607 mL 6.9017 mL
15 mM 0.1840 mL 0.9202 mL 1.8405 mL 4.6011 mL
20 mM 0.1380 mL 0.6902 mL 1.3803 mL 3.4508 mL
25 mM 0.1104 mL 0.5521 mL 1.1043 mL 2.7607 mL
30 mM 0.0920 mL 0.4601 mL 0.9202 mL 2.3006 mL
40 mM 0.0690 mL 0.3451 mL 0.6902 mL 1.7254 mL
50 mM 0.0552 mL 0.2761 mL 0.5521 mL 1.3803 mL
60 mM 0.0460 mL 0.2301 mL 0.4601 mL 1.1503 mL
80 mM 0.0345 mL 0.1725 mL 0.3451 mL 0.8627 mL
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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.

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NS-1619
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