Overview
Alternative Name TPN
Lyophilized Powder yes
Origin Synthetic peptide
MW: 2455 Da
Purity: >98% (HPLC)
Effective concentration 10-100 nM.
Sequence ALCNCNRIIIPHMCWKKCGKK.
Modifications Disulfide bonds between Cys3-Cys14, and Cys5-Cys18. Lys21 - C-terminal amidation.
Structure
Molecular formula C106H176N34O23S5.
CAS No.: 58694-52-3
Activity Tertiapin blocks a range of inward rectifier K+ channels (Kir) in particular ROMK1 and GIRK but with no effect on Kir2 family members1. In addition, it was shown to inhibit acetylcholine induced K+ currents in the heart2,3.
References-Activity
- Jin, W. and Lu, Z. (1998) Biochemistry 37, 13291.
- Drici, M.D. et al. (2000) Br. J. Pharmacol. 131, 569.
- Kitamura, H. et al. (2000) Pharmacol. Exp. Therap. 293, 196.
Accession number
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to two weeks at 4°C or three months at -20°C.
Our bioassay
Alomone Labs Tertiapin inhibits Kir3.2 channels expressed in Xenopus oocytes.A continuous current trace recorded at a holding potential of -80 mV. Channel activation was achieved by high K+ solution perfusion. 50 nM Tertiapin (#STT-250) was applied during the period (2 minutes each) marked as a green trace.
Scientific background
Tertiapin is a 21 amino acid long toxin, originally isolated from Apis mellifera bee venom. Native and synthetic Tertiapin block a range of inward rectifier K+ channels. (Kir), in particular ROMK1 (Kir1.1, IC50 = 2 nM) and GIRK (Kir3 family, IC50 for the Kir3.1/3.4 heteromer is 8.6 nM) but with no effect on Kir2 family members1. In addition, it was shown to inhibit acetylcholine-induced K+ currents in the heart2,3.
Tertiapin is as active as Tertiapin-Q (#STT-170), a derivative of Tertiapin in which the oxidation-liable methionine is replaced by a glutamine residue4.
Target Kir1.1, Kir3.2 K+ channels
Peptide Content: 100%
Lyophilized Powder
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
Citations
