Tertiapin-Q 

Blocker of K_ir Channels（鉀通道K_ir阻斷劑）

Tertiapin has been isolated from the venom of the Honeybee  Apis mellifera. Tertiapin-Q is an oxidation-resistant mutant of the wild-type tertiapin where Methionine 13 has been replaced by a Glutamine.  blocks the inwardly rectifying K_ir1.1 (ROMK1) and K_ir3.1/3.4 (GIRK1/GIRK4 also known as IKACh) potassium channels with Kd values of around 2 nM and 8 nM respectively. also inhibits calcium-activated large conductance BK potassium channels (K_Ca1.1) in a concentration and voltage-dependent manner (IC₅₀ ~ 5 nM), in addition to inhibiting K_ir3.1/3.2 (GIRK1/GIRK2) heteromultimer potassium channels with a Kd close to 270 nM.  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. 

技術(shù)資料

氨基酸序列：

Ala-Leu-Cys³-Asn-Cys⁵-Asn-Arg-Ile-Ile-Ile-Pro-His-Gln-Cys¹⁴-Trp-Lys-Lys-Cys¹⁸-Gly-Lys-Lys-NH₂ 

二硫鍵： Cys³-Cys¹⁴ and Cys⁵-Cys¹⁸ 

長(zhǎng)度 (aa)：21 

分子式： C₁₀₆H₁₇₅N₃₅O₂₄S₄ 

分子量： 2452 Da 

外觀：White lyophilized solid 

可溶性： water and saline buffer 

CAS 號(hào)： [252198-49-5] 

來源： Synthetic  

純度： > 97 %

產(chǎn)品信息