NS 6180 |
Catalog No.GC17909
One-Click Copy Product Info
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KCa3.1 channel blocker
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 353262-04-1
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 353262-04-1 | SDF | |
| Chemical Name | 4-(3-(trifluoromethyl)benzyl)-2H-benzo[b][1,4]thiazin-3(4H)-one | ||
| Canonical SMILES | FC(F)(C1=CC(CN2C3=CC=CC=C3SCC2=O)=CC=C1)F | ||
| Formula | C16H12F3NOS | M.Wt | 323.33 |
| Solubility | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 20 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0928 mL | 15.4641 mL | 30.9282 mL |
| 5 mM | 618.6 μL | 3.0928 mL | 6.1856 mL |
| 10 mM | 309.3 μL | 1.5464 mL | 3.0928 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)