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910044-56-3

中文名稱 托肽品 Q
英文名稱 Tertiapin Q
CAS 910044-56-3
分子式 C106H175N35O24S4
分子量 2452.01
MOL 文件 910044-56-3.mol
更新日期 2026/02/25 14:05:54
910044-56-3 結(jié)構(gòu)式 910044-56-3 結(jié)構(gòu)式

基本信息

中文別名
托肽品 Q
英文別名
Teriapin Q
L-Lysinamide, L-alanyl-L-leucyl-L-cysteinyl-L-asparaginyl-L-cysteinyl-L-asparaginyl-L-arginyl-L-isoleucyl-L-isoleucyl-L-isoleucyl-L-prolyl-L-histidyl-L-glutaminyl-L-cysteinyl-L-tryptophyl-L-lysyl-L-lysyl-L-cysteinylglycyl-L-lysyl-, cyclic (3→14),(5→18)-bis(disulfide)

物理化學(xué)性質(zhì)

密度1.51±0.1 g/cm3(Predicted)
儲存條件-20°C
形態(tài)Solid
顏色White to off-white
水溶解性Soluble in water (2mg/ml)
序列Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Gln-Cys-Trp-Lys-Lys-Cys-Gly-Lys-Lys-NH2 (Disulfide bridge: Cys3-Cys14, Cys5-Cys18)

安全數(shù)據(jù)

WGK GermanyWGK 3
存儲類別11 - Combustible Solids

常見問題列表

生物活性
Tertiapin-Q 是一種高度選擇性的 GIRK1/4 異二聚體和 ROMK1 (Kir1.1) 阻斷劑。
靶點

Potassium channel

體外研究

Tertiapin-Q is a highly selective blocker of G protein-coupled inwardly rectifying potassium (GIRK1/4) heterodimer and renal outer medullary potassium channel (ROMK1, Kir 1.1 ). Tertiapin-Q is a potent and selective blocker for Kir 1.1 renal outer medullary potassium, Kir 3.1 -Kir 3.4 channels and calcium activated large conductance potassium channels (big potassium channels). The somatostatin (SS-14)-activated current is almost completely blocked (93.2±2.9%, n=5; P<0.01) by preincubation with the G protein-coupled inwardly rectifying potassium (GIRK) channel blocker Tertiapin-Q (TPN-Q).

體內(nèi)研究

Tertiapin-Q is a muscarinic acetylcholine receptor-operated K + current (I K,Ach ) blocker. After the cessation of rapid atrial pacing, the atrial effective refractory period (AERP) is unchanged during the experimental period in the rapid atrial pacing (RAP) rabbits (n=6). Bepridil (1 mg/kg, n=5 for each group), Amiodarone (10 mg/kg, n=5 for each group), Vernakalant (3 mg/kg, n=5 for each group), Ranolazine (10 mg/kg, n=6 for each group) or Tertiapin-Q (0.03 mg/kg, n=5 for each group) on the AERP in the control and RAP rabbits. Tertiapin-Q significantly prolongs the AERP at each pacing cycle length both in the control and RAP rabbits. The extents of prolonging effect of Tertiapin-Q on the AERP in the RAP rabbits are greater than those in the control animals.

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