Gap19TFA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。Gap19TFA可以防止C末端(CT)与CL的分子内相互作用。Gap19TFA不阻断GJ通道或Cx40/pannexin-1半通道。Gap19TFA对心肌具有保护作用。
货号:ajcx30702
CAS:N/A
分子式:C57H97F3N14O15
分子量：1275.46
溶解度:DMSO: 100 mg/mL (78.40 mM); H2O: 100 mg/mL (78.40 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

Gap19 TFA (iv; 25 mg/kg; 10 min before ligation) significantly reduces the infarct size by approximately one-fifth[2]. Animal Model: C57/BL6 mice[2]

[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.