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Purity: ≥98%
NS1643 is a novel and potent human ether-a-go-go related gene (hERG) KV11 channel activator with EC50 of 10.5 μM. In Xenopus laevis oocytes, NS1643 increased both steady-state and tail current at all voltages tested. The EC(50) value for HERG channel activation was 10.5 microM. NS1643 also activates the ERG2 channel; however, the molecular mechanism of the activation differs between the ERG1 and ERG2 channels. For ERG2, NS1643 causes a left-ward shift of the activation curve, a faster time-constant of activation and a slower time-constant of inactivation as well as an increased relative importance for the fast component of deactivation to the total deactivation. In contrast, for ERG1, NS1643 causes a right-ward shift in the voltage-dependent release from inactivation but does not affect time-constants of deactivation.
| ln Vitro |
Oocytes' hERG currents are dose- and voltage-dependently increased by NS1643 (0-100 μM) [1]. Within the test voltage range, NS1643 (3, 10 and 30 μM) decreases the degree of rectification of hERG channels and slows down the rate of hERG inactivation [1]. MDA-MB-231 and SKBR3 cancer cells' migration and invasion are dose-dependently inhibited by NS1643 (10 and 50 μM) [2].
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| ln Vivo |
NS1643 (6 mg/kg; administered intraperitoneally twice a week) prevents the spread of breast tumors [2].
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: MDA-MB-231, SKBR3 and MCF7 breast cancer cell lines Tested Concentrations: 50 μM Incubation Duration: 24 h Experimental Results: diminished Vimentin, N-cadherin and CD44 levels, and increased E-cadherin in breast cancer cell lines. |
| Animal Protocol |
Animal/Disease Models: NSG mice with human-derived TNBC tumor xenografts[2]
Doses: 6 mg/kg Route of Administration: intraperitoneal (ip)injection; 6 mg/kg; twice per week Experimental Results: Dramatically decreased tumor growth and the metastatic liver tumors were Dramatically smaller than those in the control group. diminished levels of human nuclear antigen (HNA). |
| References |
[1]. Casis O, et al. Mechanism of action of a novel human ether-a-go-go-related gene channel activator. Mol Pharmacol. 2006 Feb;69(2):658-65. Epub 2005 Nov 11.
[2]. Breuer EK, et al. Potassium channel activity controls breast cancer metastasis by affecting β-catenin signaling. Cell Death Dis. 2019 Feb 21;10(3):180. |
| Molecular Formula |
C₁₅H₁₀F₆N₂O₃
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| Molecular Weight |
380.24
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| Exact Mass |
380.06
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| Elemental Analysis |
C, 47.38; H, 2.65; F, 29.98; N, 7.37; O, 12.62
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| CAS # |
448895-37-2
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
O=C(NC1=CC(C(F)(F)F)=CC=C1O)NC2=CC(C(F)(F)F)=CC=C2O
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.57 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6299 mL | 13.1496 mL | 26.2992 mL | |
| 5 mM | 0.5260 mL | 2.6299 mL | 5.2598 mL | |
| 10 mM | 0.2630 mL | 1.3150 mL | 2.6299 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 Time course of HERG channel activation by NS1643.
Concentration-response relationship of NS1643.Mol Pharmacol.2006 Jan;69(1):266-77. |
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NS1643 inhibits KCNQ1 current.Mol Pharmacol.2006 Jan;69(1):266-77. |
Specificity of NS1643.Mol Pharmacol.2006 Jan;69(1):266-77. |
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