Cas No.: | 1507930-57-5 |
Chemical Name: | Gap19 |
Synonyms: | Gap19;(2S)-6-Amino-2-[[(2S)-2-[[(2S)-6-amino-2-[[(2S)-6-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S)-5-;Gap19 |
SMILES: | O=C([C@H]([C@@H](C)CC)NC([C@H](CCC(=O)O)NC([C@H]([C@@H](C)CC)NC([C@H](CCC(N)=O)NC([C@H](CCCCN)N)=O)=O)=O)=O)N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(=O)O)CCCCN)=O)CC1C=CC=CC=1)=O)CCCCN)=O)CCCCN |
Formula: | C55H96N14O13 |
M.Wt: | 1161.43675327301 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Gap19, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 has protective effects against myocardial[1][2]. |
Target: | Cx43 Hemichannel[1] |
In Vivo: | Gap19 (iv; 25 mg/kg; 10 min before ligation) significantly reduces the infarct size by approximately one-fifth[2]. 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. |
In Vitro: | Gap19 (250 μM; for 30 min ) decreases mitochondrial potassium uptake[1]. Gap19 (400 μM) inhibits unitary hemichannel currents in HeLa-Cx43 cells[2]. Gap19 (100 μM) inhibits hemichannel unitary currents in ventricular cardiomyocytes[2]. Gap19 (250 μM, 30 min) protects against myocardial ischemia/reperfusion injury in vitro and in vivo[2]. |
References: | [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. |