| CAS | 58694-52-3 |
| Sequence | H-Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Met-Cys-Trp-Lys-Lys-Cys-Gly-Lys-Lys-NH2 (Disulfide bonds between Cys3 and Cys14/Cys5 and Cys18) |
| Sequence Single | ALCNCNRIIIPHMCWKKCGKK-NH2 |
| Molecular Formula | C106H176N34O23S5 |
| Molecular Weight | 2455.11 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Application | Ion Channel Modulating Agents |
| Description | Tertiapin (TPN) is a potent inhibitor of the inward-rectifier K+ channels, it blocked a G-protein-gated channel (GIRK1/4) and the ROMK1 channel with nanomolar affinities, however a closely related channel, IRK1, was insensitive to tertiapin. Thus, tertiapin will be a powerful ligand for purifying functional channels as well as for screening pharmaceutical agents against these channels. |
| References | 1. A new fluorogenic substrate for plasmin. P.A.Pierzchala et al., Biochem. J., 183, 555 (1979) 2. Tertiapin potently and selectively blocks muscarinic K(+) channels in rabbit cardiac myocytes. H.Kitamura et al., J. Pharmacol. Exp. Ther., 293, 196 (2000) 3. Tertiapin, a selective IKACh blocker, terminates atrial fibrillation with selective atrial effective refractory period prolongation. N.Hashimoto et al., Pharmacol. Res., 54, 136 (2006) |