gap 19

Tat-Gap 19, a peptide inhibitor of connexin43 (Cx43) hemichannels, is derived from the HIV-1 Tat protein transduction domain fused with a nine-amino acid sequence from Cx43 residues 128-136. This compound, at a concentration of 10 µM, effectively suppresses glutamate-induced ATP release in primary rat hepatocytes, indicating inhibition of Cx43 hemichannel activity. Furthermore, Tat-Gap 19 demonstrates therapeutic potential by significantly reducing infarct volume in a mouse cerebral ischemia-reperfusion injury model following middle cerebral artery occlusion (MCAO) at a dosage of 25 mg/kg. Moreover, its intraperitoneal administration at 1 mg/kg per day ameliorates fibrosis and decreases the area of hepatic stellate cells, the precursors to myofibroblasts, expressing α-smooth muscle actin (α-SMA), in a model of thioacetamide-induced liver damage. Additionally, it enhances superoxide dismutase (SOD) activity in hepatic cells from the treated mice, indicating its antioxidative benefits.

TAT-Gap19 acetate is a specific inhibitor of connexin43 hemichannel (Cx43 HC). TAT-Gap19 acetate traverses the blood-brain barrier and alleviates liver fibrosis in mice. TAT-Gap19 acetate does not inhibit the corresponding Cx43 GJCs.

Gap19 TFA is a selective and potent blocker of connexin 43 (Cx43) hemichannels, originating from nine amino acids within the Cx43 cytoplasmic loop (CL). It operates by hindering intramolecular interactions between the C-terminus (CT) and the CL, effectively inhibiting hemichannel activity without affecting GJ channels or Cx40/pannexin-1 hemichannels. This peptide offers protective benefits for the myocardium.

TAT-Gap19 TFA, a Cx mimetic peptide and specific connexin43 hemichannel (Cx43 HC) inhibitor, does not inhibit the corresponding Cx43 gap junction channels (GJCs). It crosses the blood-brain barrier and has been shown to alleviate liver fibrosis in mice [1] [2] [3].

Gap19 is a peptide that corresponds to a sequence on the cytoplasmic loop (CL) of Cx43.

Cx43 hemichannel blocker (IC50 ~7 μM). No significant affinity for gap junctions or Panx1 channels. N-terminal transactivator of transcription (TAT) motif promotes membrane permeability and increases inhibitory effect of Gap19. Active in vivo. Brain penet

Gap19 TFA is a peptide derived from nine amino acids of Cx43 cytoplasmic ring (CL), an effective, selective connexin 43 (Cx43) half-channel blocker.