Asc-432 Tertiapin Q

Biological Description

Potent blocker of inward rectifier K⁺ channels. Stable analogue of the bee venom tertiapin. High affinity for ROMK1 and GIRK1/4 (K_i values are 1.3 nM and 13.3 nM respectively). Displays >250-fold selectivity over many other Kir subtypes.

Useful References

Jin et al (1999) Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q. Biochemistry. 38:14294-301. abstract



Ram et al (2008) Engineered specific and high-affinity inhibitor for a subtype of inward-rectifier K+ channels. Proc Natl Acad Sci USA. 105:10774-8. abstract



Kanjhan et al (2005) Tertiapin-Q blocks recombinant and native large conductance K+ channels in a use-dependent manner. J Pharmacol Exp Ther. 314:1353-61. abstract



 

Chemical Information

ALCNCNRIIIPHQCWKKCGKK-NH2 (disulfide bridge 3-14, 5-18)

• Desiccate at -20°C


• MW 2452.01


• C₁₀₆H₁₇₅N₃₅O₂₄S₄


• 252198-49-5