Tertiapin Q (trifluoroacetate salt) (Synonyms: TPN(M13Q), TPNQ) |
| Catalog No.GC52354 |
A peptide derivative of tertiapin
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Sample solution is provided at 25 µL, 10mM.
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Tertiapin Q is a peptide derivative of the honeybee venom peptide and inhibitor of inwardly rectifying potassium (Kir) channels, tertiapin.1 It inhibits heteromultimeric potassium channels composed of G protein-activated inward rectifier potassium channel 1 (GIRK1) and GIRK4, also known as Kir3.1 and Kir3.4, respectively, as well as the inward-rectifier potassium channel 1 (Kir1.1; Kis = 13.3 and 1.3 nM, respectively).2 Tertiapin Q inhibits voltage-stimulated hyperpolarization and increases action potential duration in mouse dorsal root ganglion neurons in a concentration-dependent manner.3 It inhibits BK-type potassium channels in Xenopus oocytes expressing the human BK channel α subunit (IC50 = 5.8 nM).
1.Jin, W., Klem, A.M., Lewis, J.H., et al.Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-QBiochemistry38(43)14294-14301(1999) 2.Jin, W., and Lu, Z.Synthesis of a stable form of tertiapin: A high-affinity inhibitor for inward-rectifier K+ channelsBiochemistry38(43)14286-14293(1999) 3.Kanjhan, R., Coulson, E.J., Adams, D.J., et al.Tertiapin-Q blocks recombinant and native large conductance K+ channels in a use-dependent mannerJ. Pharmacol. Exp. Ther.314(3)1353-1361(2005)
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