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.
Chemical Formula: C16H12F3NOS
Exact Mass: 323.05917
Molecular Weight: 323.33
Elemental Analysis: C, 59.44; H, 3.74; F, 17.63; N, 4.33; O, 4.95; S, 9.92
Chemical Name: 4-[[3-(Trifluoromethyl)phenyl]methyl]-2H-1,4-benzothiazin-3(4H)-one
InChi Code: 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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
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.
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.
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.
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