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.
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- CAS. Nr.: 185855-91-8
- Formel: C21H24N2
- Molecular Weight:304.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Kv1.3 200 nM (IC50) |
Kv1.4 |
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.
Chemical Information
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CAS. Nr. 185855-91-8
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Molecular Weight 304.43
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Formel C21H24N2
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SMILES
CCCCC/N=C1C=CN(CC2=CC=CC=C2)C3=C/1C=CC=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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