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Tertiapin Q
Cat. No. KC-010
Structure:
H-Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Gln-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:
TPNQ, TPN(Q)
Activity:
Inward rectifier K+ channel blocker
Tertiapin-Q is a high affinity blocker of inward-rectifier K+ channels. Tertiapin-Q is a stable derivative of the bee venom toxin tertiapin where the methionine residue at position 13 has been replaced with glutamine, which is far less susceptible to oxidation by air. Tertiapin-Q and native tertiapin have very similar pharmacologucal properties. Tertiapin-Q also binds to ROMK1 (Kir1.1) and GIRK1/4 (Kir3.1/3.4) channels with high affinity (Ki values are 1.3 and 13.3 nM respectively) and shows selectivity over Kir2.1 channels.
Jin and Lu (1999) Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels. Biochemistry 38 14286 PMID: 10572003
Jin et al (1999) Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q. Biochemistry 38 14294 PMID: 10572004
Kanjhan et al (2005) Tertiapin-Q blocks recombinant and native large conductance K+ channels in a use-dependent manner. J Pharmacol Exp Ther. 314(3) 1353 PMID: 15947038
Related areas
All peptides >
All potassium channel modulators >
All cardiovascular research areas >
All neuroscience research categories >
Technical Data
| Structure | H-Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Gln-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 | 910044-56-3 |
| Molecular Weight | 2452 |
| Formula | C106H175N35O24S4 |
| Sequence | ALCNCNRIIIPHQCWKKCGKK-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 to 2 mg/ml in water |
| Appearance | Freeze dried solid |
| Storage | Store dry, frozen and in the dark |
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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