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Chemical Structure| 153587-01-0 Chemical Structure| 153587-01-0

Structure of NS-1619
CAS No.: 153587-01-0

Chemical Structure| 153587-01-0

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NS-1619 is a selective large conductance Ca2+-activated K+-channel activator.

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Product Details of NS-1619

CAS No. :153587-01-0
Formula : C15H8F6N2O2
M.W : 362.23
SMILES Code : OC1=C(C=C(C=C1)C(F)(F)F)N1C(=O)NC2=C1C=CC(=C2)C(F)(F)F
MDL No. :MFCD00928190
InChI Key :YLFMCMWKHSDUCT-UHFFFAOYSA-N
Pubchem ID :4552

Safety of NS-1619

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
TALL-1 cells 25 µM 45 minutes Increased mitochondrial ROS accumulation Cell Death Dis. 2018 Aug 1;9(8):822
Rat portal vein smooth muscle cells 33 µM 10 minutes To investigate the effects of NS1619 on calcium currents in rat portal vein smooth muscle cells, it was found that 33 μM NS1619 completely inhibited calcium currents within 10 minutes. Br J Pharmacol. 1994 Dec;113(4):1538-47
PDX cells 25 µM NS1619 + 100 µM DHEA 45 minutes Significantly increased mitochondrial ROS accumulation Cell Death Dis. 2018 Aug 1;9(8):822
Hippocampal neurones 1 µM 5 minutes Mimicked the actions of leptin, inhibiting the enhanced Ca2+ levels following Mg2+ removal J Physiol. 2002 Dec 15;545(3):933-44
Rat vascular smooth muscle cells 20 µM 6 days NS1619 significantly alleviated β-GP-induced vascular calcification by decreasing calcium content and alkaline phosphatase activity, reducing mRNA expression of osteogenic genes OCN and OPN, and increasing α-SMA protein expression Acta Pharmacol Sin. 2022 Mar;43(3):624-633.
Rat portal vein smooth muscle cells 10-33 µM about 6 minutes To investigate the effects of NS1619 on the currents in rat portal vein smooth muscle cells, it was found that NS1619 induced a noisy, outward current which reached a maximum within about 6 min and exhibited time-dependent activation and marked outward rectification. Br J Pharmacol. 1994 Dec;113(4):1538-47

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD/SCID mice PDX19 xenograft model Intraperitoneal injection 0.1 mg/kg NS1619 + 15 mg/kg DEX Every second day Significantly reduced PDX19 cell growth Cell Death Dis. 2018 Aug 1;9(8):822
C57BL/6 mice Healthy mice Intraperitoneal injection 1 mg/kg Single dose NS-1619 increased acute gastrointestinal uptake of 223Ra, with stomach uptake at 15 min being 2-fold higher than control, while reducing bone uptake. J Nucl Med. 2021 Apr 9;62(12):1751–8
Sprague-Dawley rats Chronic hypoxia-induced pulmonary hypertension model Perfusion 3/30/150 μM Single dose NS1619-induced vasodilation was significantly greater in hypoxic lungs, mediated by activation of BKCa channels, other TEA-sensitive K+ channels, and L-type Ca2+ channels Lung. 2014 Oct;192(5):811-7

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.76mL

0.55mL

0.28mL

13.80mL

2.76mL

1.38mL

27.61mL

5.52mL

2.76mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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