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Products
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- Technical support
- Resources
Tertiapin
Cat. No. KC-020
Structure:
H-Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Met-Cys-Trp-Lys-Lys-Cys-Gly-Lys-Lys-NH2; disulphide bridges between Cys-3 and Cys-14 and Cys-5 and Cys-18
Other Names:
TPN
Activity:
Selective IKACh blocker
Tertiapin is a peptide found in the venom of the European honey bee (Apis mellifera). Tertiapin is a selective inhibitor of the G-protein-gated atrial K+ channel IKACh that can prolong atrial effective refractory period and terminate atrial fibrillation. Tertiapin is also a selective and potent inhibitor of muscarinic K+ channels in rabbit cardiac myocytes. The methionine residue at position 13 of tertiapin is sensitive to oxidation, reducing ability to block ion channels, so the methionine may be be substituted by glutamine in order to prevent oxidation, resulting in tertiapin-Q, which shows no functional change and is a more suitable research tool for some applications.
Gauldie et al (1976) The peptide components of bee venom. Eur J Biochem. 61(2):369 PMID: 1248464
Hashimoto et al (2006) Tertiapin, a selective IKACh blocker, terminates atrial fibrillation with selective atrial effective refractory period prolongation. Pharmacol Res. 54(2) 136 PMID: 16725344
Patel et al (2020) Structural Determinants Mediating Tertiapin Block of Neuronal Kir3.2 Channels. Biochemistry 59(7) 836 PMID: 31990535
Related areas
All peptides >
All potassium channel modulators >
All cardiovascular research categories >
Technical Data
| Structure | H-Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Met-Cys-Trp-Lys-Lys-Cys-Gly-Lys-Lys-NH2; disulphide bridges between Cys-3 and Cys-14 and Cys-5 and Cys-18 |
| CAS Number | 403843-29-8 |
| Molecular Weight | 2455.07 |
| Formula | C106H176N34O23S5 |
| Sequence | ALCNCNRIIIPHMCWKKCGKK-NH2 |
| Modifications | Disulphide bridges between C-3 and C14 and C-5 and C-18, Lys-21 is a C-terminal amide |
Solubility and Storage
| Solubility | Soluble in water to 1 mg/m |
| Appearance | Freeze dried solid |
| Storage | Store dry, frozen and in the dark. Protect from air. |
Batch Specific Data
| Purity | >95% by hplc |
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Recent citations
A new publication from the University of Ljubljana uses MCA-AVLQSGFR-Lys(Dnp)-Lys-NH2, the FRET substrate for the severe acute respiratory syndrome coronavirus main protease (SARS-CoV Mpro), to determine the inhibitory potential of plant polyphenols
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