CP-339818 

CP-339818 is a non-peptide Kv1.3 channel (IC₅₀ = 200 nM) and Kv1.4 channel blocker. CP 339818 inhibits HCN channel with IC₅₀s of 18.9 μM and 43.4 μM against HCN1 and HCN4 (high Cl^-). CP-339818 has significantly weaker blocking effects on Kv1.1, Kv1.2, Kv1.5, Kv1.6, Kv3.1-4, and Kv4.2 channels. CP-339818 selectively blocked Kv1.3, thereby inhibiting the activation process of human T cells. CP-339818 can be used to study the physiological functions of HCN and Kv channels^[1][2][3].

CP-339818 suppresses human T cell activation, suggesting that blockade of Kv1.3 alone is sufficient to inhibit this process^[1].
CP-339818 (5 μM) effectively block the remaining outward potassium current in Kv2.1^⁻/⁻ β cells, and does not significantly enhance glucose-stimulated insulin secretion (GSIS)^[2].
CP-339818 (0-100 μM)'s inhibitory effect on HCN1 and HCN4 in low-concentration of Cl^- internal solution is weakened with IC₅₀ of 26.2 and > 100 μM, , and this blocking effect is also voltage-dependent (the higher the voltage, the stronger the blocking effect)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

304.43

C₂₁H₂₄N₂

185855-91-8

CCCCC/N=C1C=CN(CC2=CC=CC=C2)C3=C/1C=CC=C3

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Novel nonpeptide agents potently block the C-type inactivated conformation of Kv1.3 and suppress T cell activation  [Content Brief]

  [2]. Jacobson DA, et al. Calcium-activated and voltage-gated potassium channels of the pancreatic islet impart distinct and complementary roles during secretagogue induced electrical responses. J Physiol. 2010 Sep 15;588(Pt 18):3525-37.  [Content Brief]

  [3]. Lee YT, et al. Novel pharmacological activity of loperamide and CP-339,818 on human HCN channels characterized with an automated electrophysiology assay. Eur J Pharmacol. 2008 Feb 26;581(1-2):97-104.  [Content Brief]