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Type HazMat fee for 500 gram (Estimated)
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Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
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Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 448895-37-2 Chemical Structure| 448895-37-2

Structure of NS1643
CAS No.: 448895-37-2

Chemical Structure| 448895-37-2

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NS-1643 is a potent human ether-a-go-go related gene (hERG) KV11.1 channel activator with EC50 of 10.5 μM.

4.5 *For Research Use Only !

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Product Details of NS1643

CAS No. :448895-37-2
Formula : C15H10F6N2O3
M.W : 380.24
SMILES Code : OC1=C(NC(=O)NC2=C(O)C=CC(=C2)C(F)(F)F)C=C(C=C1)C(F)(F)F
MDL No. :MFCD08705418
InChI Key :NJFVQMRYJZHGME-UHFFFAOYSA-N
Pubchem ID :10177784

Safety of NS1643

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301-H319
Precautionary Statements:P301+P310-P305+P351+P338
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
MCF7 50 µM 24 hours Inhibited cell migration and invasion by reversing EMT phenotype Cell Death Dis. 2019 Feb 21;10(3):180
SKBR3 50 µM 24 hours Inhibited cell migration and invasion by reversing EMT phenotype Cell Death Dis. 2019 Feb 21;10(3):180
FET cells 50 µM 16 hours Inhibits the migratory ability of FET cells Cancers (Basel). 2021 Nov 30;13(23):6025
SW480 cells 50 µM 16 hours No significant effect on the migratory ability of SW480 cells Cancers (Basel). 2021 Nov 30;13(23):6025
HT29 cells 50 µM 16 hours Inhibits the migratory ability of HT29 cells Cancers (Basel). 2021 Nov 30;13(23):6025
MDA-MB-231 50 µM 24 hours Inhibited cell migration and invasion by reversing EMT phenotype Cell Death Dis. 2019 Feb 21;10(3):180
MCF-7 cells 50 µM 24 hours NS1643 significantly reduced the phosphorylation level of exogenously expressed Cav-1. Cells. 2022 Aug 8;11(15):2461
MDA-MB-231 cells 50 µM 24 hours NS1643 significantly decreased the migratory ability of MDA-MB-231 cells. Cells. 2022 Aug 8;11(15):2461
CHO-H1 cells 0-50 µM 24-72 hours NS1643 had no effect on the proliferation rate of CHO-H1 cells Cell Death Dis. 2013 Jun 6;4(6):e652
MDA-MB-231 cells 0-50 µM 24-72 hours NS1643 significantly inhibited proliferation of MDA-MB-231 cells, leading to cell cycle arrest in G0/G1 phase, accompanied by increased protein levels of p21 and p16INK4a and positive β-galactosidase assay Cell Death Dis. 2013 Jun 6;4(6):e652
SKBr3 cells 0-50 µM 24-72 hours NS1643 significantly inhibited proliferation of SKBr3 cells, leading to cell cycle arrest in G0/G1 phase, accompanied by increased protein levels of p21 and p16INK4a and positive β-galactosidase assay Cell Death Dis. 2013 Jun 6;4(6):e652
HEK293 cells 3 µM 5 minutes To measure the effect of NS1643 on hERG current, results showed that NS1643 activated hERG current by 55% at 3 μM. Br J Pharmacol. 2008 Aug;154(7):1427-38
U87 cells 50 µM 6 days NS1643 alone significantly reduced the proliferation of U87 cells, with a 1.7-fold decrease compared to control Cancers (Basel). 2022 Mar 15;14(6):1499
NG108-15 cells 20 µM and 50 µM 6 days NS1643 alone significantly reduced the proliferation of NG108-15 cells, with a 1.6- and 2.4-fold decrease compared to control, respectively Cancers (Basel). 2022 Mar 15;14(6):1499

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rabbits Isolated Langendorff-perfused heart model Perfusion 1 μM and 10 μM 30 minutes per concentration To evaluate the effect of NS1643 on cardiac action potential and QT interval, results showed that NS1643 significantly shortened APD and QT interval, and induced ventricular fibrillation (VF) at 10 μM. Br J Pharmacol. 2008 Aug;154(7):1427-38
Rabbit Langendorff perfused heart model Perfusate 20 μM Not specified To study the effect of NS1643 on atrial T-wave alternans (Ta-wave alternans). Results showed that NS1643 significantly attenuated or completely abolished Ta-wave alternans. J Physiol. 2019 Feb;597(3):723-740
Mice Hypokalaemic murine heart model Perfusion 30 μM 20 minutes NS1643 demonstrated anti-arrhythmic efficacy in the hypokalaemic murine heart by suppressing EADs, reducing APD90, and restoring DAPD90. Acta Physiol (Oxf). 2008 May;193(1):25-36
NSG mice Triple-negative breast cancer xenograft model Intraperitoneal injection 6 mg/kg Every 2 days for 6 weeks Significantly reduced metastatic spread of breast tumors by inhibiting cell motility and reprogramming EMT via attenuation of Wnt/β-catenin signaling Cell Death Dis. 2019 Feb 21;10(3):180
Sprague Dawley rats Septic cardiac dysfunction model induced by caecal ligation puncture (CLP) surgery or lipopolysaccharide (LPS) injection Intraperitoneal injection 6 mg/kg Single administration, survival rate or cardiac function was monitored Activation of Kcnh2 with NS1643 significantly improved the survival rate of septic rats, ameliorated cardiac function, and attenuated cardiac tissue damage and cardiomyocyte apoptosis. Cell Prolif. 2021 Feb;54(2):e12962

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.15mL

2.63mL

1.31mL

26.30mL

5.26mL

2.63mL

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

 

Historical Records

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