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T8316

Sigma-Aldrich

Tertiapin

>95%

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About This Item

Empirical Formula (Hill Notation):
C106H176N34O23S5
CAS Number:
Molecular Weight:
2455.07
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.32

assay

>95%

form

powder

technique(s)

HPLC: suitable

storage temp.

−20°C

Amino Acid Sequence

Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Met-Cys-Trp-Lys-Lys-Cys-Gly-Lys-Lys-NH2

Application

Tertiapin was used for developing a novel CZE-DAD method for analyzing the honeybee venom.

Biochem/physiol Actions

A potent inhibitor of the inward-rectifier K+ channels, 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 is a tool for purifying functional channels as well as for screening pharmaceutical agents against these channels.
Tertiapin is a peptide isolated from honey bee venom, which is a selective IKACh blocker that prolongs the atrial effective refractory period and terminates the atrial fibrillation. It is a selective and potent inhibitor of muscarinic K+ channels in rabbit cardiac myocytes.

Preparation Note

Tertiapin dissolves in water at 1 mg/ml to yield a clear solution.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)


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Norio Hashimoto et al.
Pharmacological research, 54(2), 136-141 (2006-05-27)
It is well known that vagal nerve tone plays a crucial role in atrial fibrillation (AF). Acetylcholine-activated potassium current (IKACh) mediates much of the cardiac response to vagal nerve stimulation (VNS), but the contribution of IKACh to AF remains unknown.
H Kitamura et al.
The Journal of pharmacology and experimental therapeutics, 293(1), 196-205 (2000-03-29)
Tertiapin is a 21-residue peptide isolated from honey bee venoms. A recent study indicated that tertiapin is a potent blocker of certain types of inwardly rectifying K(+) (Kir) channels (). We examined the effect of tertiapin on ion channel currents
Zenon J Kokot et al.
Analytical and bioanalytical chemistry, 399(7), 2487-2494 (2011-01-12)
The aim of this study was to develop a new precise and accurate CZE-DAD method for honeybee venom analysis using cytochrome c as an internal standard. The 64.5 cm total length, 56 cm effective length, 75 μm ID, and 360
W Jin et al.
Biochemistry, 37(38), 13291-13299 (1998-09-28)
Inward-rectifier K+ channels are a group of highly specialized K+ channels that accomplish a variety of important biological tasks. Inward-rectifier K+ channels differ from voltage-activated K+ channels not only functionally but also structurally. Each of the four subunits of the

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