NS 6180KCa3.1 channel blocker CAS# 353262-04-1 |
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Quality Control & MSDS
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| Cas No. | 353262-04-1 | SDF | Download SDF |
| PubChem ID | 11837221 | Appearance | Powder |
| Formula | C16H12F3NOS | M.Wt | 323.33 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 100 mg/mL (309.28 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 4-[[3-(trifluoromethyl)phenyl]methyl]-1,4-benzothiazin-3-one | ||
| SMILES | C1C(=O)N(C2=CC=CC=C2S1)CC3=CC(=CC=C3)C(F)(F)F | ||
| Standard InChIKey | ZUIJXKLTUFCDGO-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C16H12F3NOS/c17-16(18,19)12-5-3-4-11(8-12)9-20-13-6-1-2-7-14(13)22-10-15(20)21/h1-8H,9-10H2 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Potent KCa3.1 channel blocker (IC50 values are 9, 14 and 15 nM for rat, human and mouse erythrocyte KCa3.1 channels respectively). Exhibits ~ 50% inhibition of KCa1.1, KV1.3, and KV11.1 channels, noradrenaline and dopamine transporters, L-type Ca2+ channels and melatonin receptors at a concentration of 10 μM. Potently inhibits IL-2 and IFN-γ production in rat lymphocytes (IC50 ~ 50 nM); reduces DBNS-induced experimental colitis in rats. |
NS 6180 Dilution Calculator
NS 6180 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.0928 mL | 15.4641 mL | 30.9282 mL | 61.8563 mL | 77.3204 mL |
| 5 mM | 0.6186 mL | 3.0928 mL | 6.1856 mL | 12.3713 mL | 15.4641 mL |
| 10 mM | 0.3093 mL | 1.5464 mL | 3.0928 mL | 6.1856 mL | 7.732 mL |
| 50 mM | 0.0619 mL | 0.3093 mL | 0.6186 mL | 1.2371 mL | 1.5464 mL |
| 100 mM | 0.0309 mL | 0.1546 mL | 0.3093 mL | 0.6186 mL | 0.7732 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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IC50: 9, 14 and 15 nM for rat, human and mouse erythrocyte KCa3.1 channels, respectively.
NS 6180 is a potent KCa3.1 channel blocker. KCa3.1 (the Ca2+-activated K+ channel, encoded by the KCNN4 gene) plays a key role in these processes by participating in the regulation of calcium entry.
In vitro: NS6180 blocked cloned human KCa3.1 channels via T250 and V275, while the same amino acid residues conferred sensitivity to triarylmethanes such as like TRAM-34. NS6180 blocked endogenously expressed KCa3.1 channels in human, mouse and rat erythrocytes with similar potencies. Rat and mouse splenocyte proliferation was suppressed NS6180 at submicrolar concentrations, which potently inhibited IL-2 and IFN-g production, exerting smaller effects on IL-4 and TNF-a and no effect on IL-17 production. After induction of colitis, antibody staining exhibited KCa3.1 channels in healthy colon and strong up-regulation in association with infiltrating immune cells [1].
In vivo: Despite poor plasma exposure, NS6180 (3 and 10 mg·kg-1 b.i.d.) abolished colon inflammation and improved body weight gain effectively, just as the standard IBD drug sulfasalazine (300 mg·kg-1 q.d.). The benzothiazinone NS6180 was potent on recombinant and endogenously expressed KCa3.1 channels, selectivity and molecular site of action. Furthermore, the effect of NS6180 characterize its pharmacokinetics on the activity of T-lymphocytes from wild-type and KCa3.1–/– knockout mice and show that it abolishes inflammation in an animal model of IBD [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Strbk D, Brown DT, Jenkins DP, Chen YJ, Coleman N, Ando Y, Chiu P, Jrgensen S, Demnitz J, Wulff H, Christophersen P. 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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NS6180, a new K(Ca) 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease.[Pubmed:22891655]
Br J Pharmacol. 2013 Jan;168(2):432-44.
BACKGROUND AND PURPOSE: The K(Ca) 3.1 channel is a potential target for therapy of immune disease. We identified a compound from a new chemical class of K(Ca) 3.1 inhibitors and assessed in vitro and in vivo inhibition of immune responses. EXPERIMENTAL APPROACH: We characterized the benzothiazinone NS6180 (4-[[3-(trifluoromethyl)phenyl]methyl]-2H-1,4-benzothiazin-3(4H)-one) with respect to potency and molecular site of action on K(Ca) 3.1 channels, selectivity towards other targets, effects on T-cell activation as well as pharmacokinetics and inflammation control in colitis induced by 2,4-dinitrobenzene sulfonic acid, a rat model of inflammatory bowel disease (IBD). KEY RESULTS: NS6180 inhibited cloned human K(Ca) 3.1 channels (IC(50) = 9 nM) via T250 and V275, the same amino acid residues conferring sensitivity to triarylmethanes such as like TRAM-34. NS6180 inhibited endogenously expressed K(Ca) 3.1 channels in human, mouse and rat erythrocytes, with similar potencies (15-20 nM). NS6180 suppressed rat and mouse splenocyte proliferation at submicrolar concentrations and potently inhibited IL-2 and IFN-gamma production, while exerting smaller effects on IL-4 and TNF-alpha and no effect on IL-17 production. Antibody staining showed K(Ca) 3.1 channels in healthy colon and strong up-regulation in association with infiltrating immune cells after induction of colitis. Despite poor plasma exposure, NS6180 (3 and 10 mg.kg(-1) b.i.d.) dampened colon inflammation and improved body weight gain as effectively as the standard IBD drug sulfasalazine (300 mg.kg(-1) q.d.). CONCLUSIONS AND IMPLICATIONS: NS6180 represents a novel class of K(Ca) 3.1 channel inhibitors which inhibited experimental colitis, suggesting K(Ca) 3.1 channels as targets for pharmacological control of intestinal inflammation.
