NS6180
new
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 522389

CAS#: 353262-04-1

Description: NS6180 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 Structure

img
NS6180
CAS# 353262-04-1
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 522389
Name: NS6180
CAS#: 353262-04-1
Chemical Formula: C16H12F3NOS
Exact Mass: 323.06
Molecular Weight: 323.330
Elemental Analysis: C, 59.44; H, 3.74; F, 17.63; N, 4.33; O, 4.95; S, 9.92

Price and Availability

Size Price Availability Quantity
10mg USD 90 Ready to ship
25mg USD 150 Ready to ship
50mg USD 250 Ready to ship
100mg USD 450 Ready to ship
200mg USD 750 Ready to ship
500mg USD 1250 Ready to ship
1g USD 1950 Ready to ship
2g USD 2950 Ready to ship
5g USD 4650 Ready to ship
Bulk inquiry

Related CAS #: 353262-04-1   NS6180 hydrate  

Synonym: NS6180; NS-6180; NS 6180.

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

InChi Key: ZUIJXKLTUFCDGO-UHFFFAOYSA-N

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

SMILES Code: O=C1CSC2=CC=CC=C2N1CC3=CC=CC(C(F)(F)F)=C3

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

More Info:

Biological target: NS6180 is a novel potent and selective KCa3.1 channel inhibitor (IC50 = 9 nM) that prevents T-cell activation and inflammation (IC50 = 9 nM).
In vitro activity: NS6180 is a novel potent and selective KCa3.1 channel inhibitor (IC50 = 9 nM) that prevents T-cell activation and inflammation (IC50 = 9 nM).
In vivo activity: In order to evaluate NS6180 efficacy in blocking KCa3.1 channels in a disease model, NS6180 was tested in DNBS-induced colitis in rats, a model of human IBD. In keeping with the known expression of KCa3.1 channels in intestinal epithelium (Rufo et al., 1997), immunohistochemical staining for these channels in colon sections from normal rats revealed KCa3.1 channels on the epithelial cells lining the well-aligned parallel crypts (Figure 7, upper panels) and on occasional ED1+ macrophages or CD43+ T cells in the muscularis mucosae and lamina propria (Figure 7, upper panels). In a separate series of experiments, groups of DNBS challenged rats were treated with two doses (3 and 10 mg·kg−1 b.i.d.) of NS6180 for 7 days in direct comparison with the IBD drug sulfasalazine (300 mg·kg−1 q.d.). The disease symptoms were followed, and Figure 8 shows the relative colon (Figure 8A) and body weight development (Figure 8B) of the different groups after 8 days of treatment. Both doses of NS6180 significantly improved weight gain and decreased inflammation induced swelling of the colon as determined by relative colon weight. The positive control sulfasalazine also significantly affected both body weight and colon inflammation (Figure 8). The effects of NS6180 and sulfasalazine did not differ significantly in magnitude. Br J Pharmacol. 2013 Jan; 168(2): 432–444. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3572569/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 20.0 61.90

Preparing Stock Solutions

The following data is based on the product molecular weight 323.33 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. 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. PMID: 22891655; PMCID: PMC3572569. 2. 1. 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. PMID: 22891655; PMCID: PMC3572569.
In vitro protocol: 1. 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. PMID: 22891655; PMCID: PMC3572569.
In vivo protocol: 1. 1. 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. PMID: 22891655; PMCID: PMC3572569.

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

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.