NS-1619
Based on 4 publication(s) in Google Scholar
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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- Pureza : 98.06%
- No. CAS: 153587-01-0
- Fòrmula: C15H8F6N2O2
- Peso molecular:362.23
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) NS-1619
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Actividad biológica
Descripciòn
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. Further protocols information, click here.
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Cell Line:The human ovarian cancer cell line A2780
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Concentration:5, 10, 30, 50, and 100 μM
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Incubation Time:48 hours
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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.
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Cell Line:A2780 cells
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Concentration:0, 5, 10, 30, 50, and 100 μM
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Incubation Time:48 hours
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Result:Expression of p53, p21, and Bax in A2780 cells was significantly increased in comparison with control.
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Cell Line:A2780 cells
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Concentration:30 μM
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Incubation Time:36 and 48 hours
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male outbred ICR mice[3]
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Dosage:1 mg/kg
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Administration:Pretreated i.p. 24 h before I/R
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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%.
Chemical Information
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No. CAS 153587-01-0
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Appearance Solid
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Peso molecular 362.23
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Fòrmula C15H8F6N2O2
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Color White to off-white
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SMILES
O=C1NC2=CC(C(F)(F)F)=CC=C2N1C3=CC(C(F)(F)F)=CC=C3O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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J Clin Invest
Potentiation of BKCa channels by cystic fibrosis transmembrane conductance regulator (CFTR) correctors VX-445 and VX-121. [Abstract]2024 Jul 2;134(16):e176328. PMID: 38954478 -
Cell Calcium
2026 Mar:134:103117. PMID: 41539212 -
J Cell Physiol
BKCa channel participates in insulin-induced lipid deposition in adipocytes by increasing intracellular calcium. [Abstract]2021 Aug;236(8):5818-5831. PMID: 33432604 -
bioRxiv
Neuronal potassium channel activity triggers initiation of mRNA translation through binding of translation regulators. [Abstract]2024 Feb 7:2024.02.07.579306. PMID: 38370631
Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. H Yamamura, et al. BK channel activation by NS-1619 is partially mediated by intracellular Ca2+ release in smooth muscle cells of porcine coronary artery. Br J Pharmacol. 2001 Feb;132(4):828-34. [Content Brief]
[2]. Xiaobing Han,et al. The potassium ion channel opener NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells. Biochem Biophys Res Commun. 2008 Oct 17;375(2):205-9. [Content Brief]
[3]. Xiaoyin Wang, et al. Opening of Ca2+-activated K+ channels triggers early and delayed preconditioning against I/R injury independent of NOS in mice. Am J Physiol Heart Circ Physiol. 2004 Nov;287(5):H2070-7. [Content Brief]
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 |
NS-1619 Related Classifications
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