Tertiapin Q

110 468 


Blocker of Kir Channels

Tertiapin has been isolated from the venom of the Honeybee Apis melliferaTertiapin-Q is an oxidation-resistant mutant of the wild-type tertiapin where Methionine 13 has been replaced by a Glutamine. Tertiapin-Q blocks the inwardly rectifying Kir1.1 (ROMK1) and Kir3.1/3.4 (GIRK1/GIRK4 also known as IKACh) potassium channels with Kd values of around 2 nM and 8 nM respectively.Tertiapin-Q also inhibits calcium-activated large conductance BK potassium channels (KCa1.1) in a concentration and voltage-dependent manner (IC50 ~ 5 nM), in addition to inhibiting Kir3.1/3.2 (GIRK1/GIRK2) heteromultimer potassium channels with a Kd close to 270 nM. Tertiapin-Q can prevent dose-dependent acetylcholine(ACh)-induced atrioventricular blocks in mammalian hearts, as KCNJ3/KCNJ5 channels (also named I(KACh)), are activated by ACh found in mammalian myocytes.

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AA sequence: Ala-Leu-Cys3-Asn-Cys5-Asn-Arg-Ile-Ile-Ile-Pro-His-Gln-Cys14-Trp-Lys-Lys-Cys18-Gly-Lys-Lys-NH2
Disulfide bonds: Cys3-Cys14 and Cys5-Cys18
Length (aa): 21
Formula: C106H175N35O24S4
Molecular Weight: 2452 Da
Appearance: White lyophilized solid
Solubility: water and saline buffer
CAS number: [252198-49-5] Source: Synthetic
Purity rate: > 97 %

Characterization of Kir1.1 channels with the use of a radiolabeled derivative of tertiapin,Biochemistry

Tertiapin-Q blocks recombinant and native large conductance K+ channels in a use-dependent manner

Titration of tertiapin-Q inhibition of ROMK1 channels by extracellular protons

Tertiapin potently and selectively blocks muscarinic K(+) channels in rabbit cardiac myocytes

Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q, Biochemistry

Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels


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    Tertiapin Q

    110 468 Quote request