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.
For research use only. We do not sell to patients.
- CAS No.: 185855-91-8
- Formula: C21H24N2
- Molecular Weight:304.43
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
Kv1.3 200 nM (IC50) |
Kv1.4 |
In Vitro
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. Further protocols information, click here.
Chemical Information
-
CAS No. 185855-91-8
-
Molecular Weight 304.43
-
Formula C21H24N2
-
SMILES
CCCCC/N=C1C=CN(CC2=CC=CC=C2)C3=C/1C=CC=C3
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CP-339818 Related Classifications
HY-114540 Related Classifications
Powered by Bioz