NS-6180

NS6-180 is a potent KCa3.1 channel blocker (IC50 values are 9, 14 and 15 nM for rat, human and mouse erythrocyte KCa3.1 channels respectively). NS6180 prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. NS6180 shows ~ 50% inhibition of KCa1.1, KV1.3, and KV11.1 channels, 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.

Product information

CAS Number: 353262-04-1

Molecular Weight: 323.33

Formula: C16H12F3NOS

Synonym:

NS 6180

NS6180

NS-6180

Related CAS Number:

353262-04-1 (hydrate)

Chemical Name: 4-[[3-(Trifluoromethyl)phenyl]methyl]-2H-1,4-benzothiazin-3(4H)-one

Smiles: O=C1CSC2=CC=CC=C2N1CC1C=C(C=CC=1)C(F)(F)F

InChiKey: ZUIJXKLTUFCDGO-UHFFFAOYSA-N

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

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO, not in water

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

References:

1. Jenkins DP, Yu W, Brown BM, Løjkner LD, Wulff H. Development of a QPatch automated electrophysiology assay for identifying KCa3.1 inhibitors and activators. Assay Drug Dev Technol. 2013 Nov-Dec;11(9-10):551-60. doi: 10.1089/adt.2013.543. PubMed PMID: 24351043; PubMed Central PMCID: PMC3870577.
2. Koshy S, Wu D, Hu X, Tajhya RB, Huq R, Khan FS, Pennington MW, Wulff H, Yotnda P, Beeton C. Blocking KCa3.1 channels increases tumor cell killing by a subpopulation of human natural killer lymphocytes. PLoS One. 2013 Oct 11;8(10):e76740. doi: 10.1371/journal.pone.0076740. eCollection 2013. PubMed PMID: 24146918; PubMed Central PMCID: PMC3795664.
3. Jørgensen S, Dyhring T, Brown DT, Strøbæk D, Christophersen P, Demnitz J. A high-throughput screening campaign for detection of ca(2+)-activated k(+) channel activators and inhibitors using a fluorometric imaging plate reader-based tl(+)-influx assay. Assay Drug Dev Technol. 2013 Apr;11(3):163-72. doi: 10.1089/adt.2012.479. Epub 2012 Nov 30. PubMed PMID: 23198866.
4. Strøbæk D, Brown DT, Jenkins DP, Chen YJ, Coleman N, Ando Y, Chiu P, Jørgensen 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. doi: 10.1111/j.1476-5381.2012.02143.x. PubMed PMID: 22891655; PubMed Central PMCID: PMC3572569.

Products are for research use only. Not for human use.