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.
性状
Solid
IC50 & Target[1][2]
Cx43 Hemichannel
体外研究(In Vitro)
Gap19 TFA (250 μM; for 30 min ) decreases mitochondrial potassium uptake. Gap19 TFA (400 μM) inhibits unitary hemichannel currents in HeLa-Cx43 cells. Gap19 TFA (100 μM) inhibits hemichannel unitary currents in ventricular cardiomyocytes. Gap19 TFA (250 μM, 30 min) protects against myocardial ischemia/reperfusion injury in vitro and in vivo. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: C57/BL6 mice
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Sealed storage, away from moisturePowder -80°C 2 years;-20°C 1 year
SequenceShortening
KQIEIKKFK
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.
溶解度数据
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