Gap19 TFA

Gap19 TFA; 纯度: 95.11%

Gap19 TFA 是一种衍生自 Cx43 细胞质环 (CL) 九个氨基酸的肽,一种有效的,选择性连接蛋白 43 (Cx43) 半通道阻滞剂。Gap19 TFA 可以防止 C 末端 (CT) 与 CL 的分子内相互作用。Gap19 TFA 不阻断 GJ 通道或 Cx40/pannexin-1 半通道。Gap19 TFA 对心肌具有保护作用。

Gap19 TFAamp;;

Gap19 TFA Chemical Structure

规格 价格 是否有货 数量
1 mg ¥1500 In-stock
5 mg ¥4500 In-stock
10 mg ¥7500 In-stock
50 mg ; 询价 ;
100 mg ; 询价 ;

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Gap19 TFA 相关产品

bull;相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cardiovascular Disease Compound Library
  • Cytoskeleton Compound Library
  • Peptide Library

生物活性

Gap19 TFA, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 TFA inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 TFA is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 TFA has protective effects against myocardial[1][2].

IC50 Target

Cx43 Hemichannel[1]

体外研究
(In Vitro)

Gap19 TFA (250 μM; for 30 min ) decreases mitochondrial potassium uptake[1].
Gap19 TFA (400 μM) inhibits unitary hemichannel currents in HeLa-Cx43 cells[2].
Gap19 TFA (100 μM) inhibits hemichannel unitary currents in ventricular cardiomyocytes[2].
Gap19 TFA (250 μM, 30 min) protects against myocardial ischemia/reperfusion injury in vitro and in vivo[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Gap19 TFA (iv; 25 mg/kg; 10 min before ligation) significantly reduces the infarct size by approximately one-fifth[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57/BL6 mice[2]
Dosage: 25 mg/kg
Administration: IV; 10 min before ligation
Result: Significantly reduced the infarct size by approximately one-fifth.

分子量

1275.46

Formula

C57H97F3N14O15

Sequence Shortening

KQIEIKKFK

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro:;

DMSO : 100 mg/mL (78.40 mM; Need ultrasonic)

H2O : 100 mg/mL (78.40 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.7840 mL 3.9202 mL 7.8403 mL
5 mM 0.1568 mL 0.7840 mL 1.5681 mL
10 mM 0.0784 mL 0.3920 mL 0.7840 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Boengler K, et al. Connexin 43 impacts on mitochondrial potassium uptake. Front Pharmacol. 2013 Jun 6;4:73.

    [2]. Wang N, et al. Selective inhibition of Cx43 hemichannels by Gap19 and its impact on myocardial ischemia/reperfusion injury. Basic Res Cardiol. 2013 Jan;108(1):309.