| CAS | 910044-56-3 |
| Sequence | H-Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Gln-Cys-Trp-Lys-Lys-Cys-Gly-Lys-Lys-NH2(Disulfide bonds between Cys3 and Cys14/Cys5 and Cys18) |
| Sequence Single | ALCNCNRIIIPHQCWKKCGKK-NH2 |
| Molecular Formula | C106H175N35O24S4 |
| Molecular Weight | 2452.04 |
| Synonyms | TPNQ, Tertiapin (M13Q), (Gln13)-Tertiapin |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Application | Ion Channel Modulating Agents |
| Description | Tertiapin Q also called TPNQ, Tertiapin (M13Q), (Gln13)-Tertiapin, shows the same channel-blocking activity as the bee venom peptide tertiapin, but increased stability due to the exchange of Met13 by Gln. Tertiapin-Q is a highly selective blocker of GIRK1/4 heterodimer and ROMK1 (Kir1.1). |
| References | 1. Non-hydrogen-bonded secondary structure in beta-peptides: evidence from circular dichroism of (S)-pyrrolidine-3-carboxylic acid oligomers and (S)-nipecotic acid oligomers. B.R.Huck et al., Org. Lett., 1, 1717 (1999) 2. Tertiapin-Q removes a large and rapidly acting component of vagal slowing of the guinea-pig cardiac pacemaker. C.P.Bolter et al., Auton. Neurosci., 150, 76 (2009) 3. The effects of tertiapin-Q on responses of the sinoatrial pacemaker of the guinea-pig heart to vagal nerve stimulation and muscarinic agonists. C.P.Bolter et al., Exp. Physiol., 93, 53 (2008) 4. Tertiapin-Q blocks recombinant and native large conductance K+ channels in a use-dependent manner. R.Kanjhan et al., J. Pharmacol. Exp. Ther., 314, 1353 (2005) 5. Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q. W.Jin et al., Biochemistry, 38, 14294 (1999) 6. A novel high-affinity inhibitor for inward-rectifier K+ channels. W.Jin and Z.Lu, Biochemistry, 37, 13291 (1998) 7. Mechanisms underlying the endogenous dopaminergic inhibition of spinal locomotor circuit function in Xenopus tadpoles. Picton LD, et al. Sci Rep. 2016 Oct 20;6:35749. 8. Research Resource: Real-Time Analysis of Somatostatin and Dopamine Receptor Signaling in Pituitary Cells Using a Fluorescence-Based Membrane Potential Assay. Günther T, et al. Mol Endocrinol. 2016 Apr;30(4):479-90. 9. Influences of rapid pacing-induced electrical remodeling on pharmacological manipulation of the atrial refractoriness in rabbits. Chiba T, et al. J Pharmacol Sci. 2016 Mar;130(3):170-6. |