NS6180

SKU: orb1225225

Description

NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.

Key Properties

• CAS Number: 353262-04-1
• MW: 323.33
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₂F₃NOS
• SMILES: O=C1CSC2=CC=CC=C2N1CC3=CC=CC(C(F)(F)F)=C3
• Target: Potassium Channel
• Solubility: DMSO: 100 mM

Bioactivity

• In Vivo:
  NS6180 (i. v. , i.p. and oral administration; 10 mg/kg; twice daily or once daily) has extremely low bioavailability and reduces DNBS-induced experimental colitis in rats. Animal model: Rats. Dosage: 10 mg/kg. Administration: i. v. , i.p. and oral administration; 10 mg/kg; twice daily or once daily. Result: Had a plasma half-life of 3.8 h, oral or i.p. administration gave low plasma exposure (Cmax: 186 nM and 33 nM, respectively, after administration of 10 mg/kg).
• In Vitro:
  NS6180 (0.001-1 μM) shows inhibition of human KCa3.1 with an IC50 value of 9.4 nM and a K50 value of 11 1.7 nM, respectively. NS6180 (30 nM, 10 μM) has inhibition that dependent on amino acid residues T250 and V275.NS6180 (1, 10, 100 and 1000 nM; 1 min) shows CCCPreportedhyperpolarizations of human erythrocytes. NS6180 (1, 10, 100 and 1000 nM; 1 min) blocks the erythrocyte KCa3.1 channels with IC50 values of 14 nM (human KCa3.1 channels), 15 nM (mouse) and 9 nM (rats), respectively. NS6180 (0-5 μM, 48 h) suppresses rat and mouse splenocyte proliferation at submicrolar concentrations and potently inhibited IL-2 and IFN-g production, while exerting smaller effects on IL-4 andTNF-α and no effect on IL-17 production.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NS6180 | NS-6180 | NS 6180

Quick Database Links

Gene Symbol

Potassium Channel