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NS6180 is a novel potent and selective KCa3.1 channel inhibitor with IC50 of 9 nM. KCa3.1 channels are targets for pharmacological control of intestinal inflammation. NS6180 prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. NS6180 inhibited cloned human KCa3.1 channels via T250 and V275, the same amino acid residues conferring sensitivity to triarylmethanes such as like TRAM-34. NS6180 inhibited endogenously expressed KCa3.1 channels in human, mouse and rat erythrocytes, with similar potencies (15–20 nM).
| ln Vitro |
Human KCa3.1 is inhibited by NS6180 (0.001–1 μM), with an IC50 of 9.4 nM and a K50 of 11 1.7 nM, respectively[1]. The inhibition of NS6180 (30 nM, 10 μM) is reliant on the amino acid residues T250 and V275[1]. Human erythrocytes with CCCP-reported hyperpolarizations are shown in NS6180 (1, 10, 100, and 1000 nM; 1 min)[1]. With IC50 values of 14 nM for human KCa3.1 channels, 15 nM for mouse KCa3.1 channels, and 9 nM for rat KCa3.1 channels, respectively, NS6180 (1, 10, 100, and 1000 nM; 1 min) blocks the erythrocyte KCa3.1 channels[1]. NS6180 (0-5 μM, 48 h) potently inhibits the production of IL-2 and IFN-g and suppresses the proliferation of rat and mouse splenocytes at submicrolar concentrations; it has no effect on the production of IL-17 and has smaller effects on IL-4 and TNF-α[1].
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| ln Vivo |
With its extremely low bioavailability, NS6180 (iv, ip, and oral administration; 10 mg/kg; twice daily or once daily) helps rats with DNBS-induced experimental colitis[1].
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| Animal Protocol |
Animal/Disease Models: Rats[1]
Doses: 10 mg/kg Route of Administration: iv, ip and oral administration; 10 mg/kg; twice (two times) daily or one time/day Experimental Results: Had a plasma half-life of 3.8 h, oral or ip administration gave low plasma exposure (Cmax: 186 nM and 33 nM, respectively, after administration of 10 mg/kg). |
| References |
[1]. Strobak D, et al. NS6180, a new K(Ca) 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. Br J Pharmacol. 2013 Jan;168(2):432-44.
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| Molecular Formula |
C₁₆H₁₂F₃NOS
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| Molecular Weight |
323.33
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| Exact Mass |
323.06
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| Elemental Analysis |
C, 59.44; H, 3.74; F, 17.63; N, 4.33; O, 4.95; S, 9.92
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| CAS # |
353262-04-1
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
S1C([H])([H])C(N(C2=C([H])C([H])=C([H])C([H])=C12)C([H])([H])C1C([H])=C([H])C([H])=C(C(F)(F)F)C=1[H])=O
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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 (7.73 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 (7.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0928 mL | 15.4641 mL | 30.9282 mL | |
| 5 mM | 0.6186 mL | 3.0928 mL | 6.1856 mL | |
| 10 mM | 0.3093 mL | 1.5464 mL | 3.0928 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.
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