To investigate the inhibitory effect of Gap19 on Cx43 hemichannels, results showed that Gap19 significantly reduced unitary current activities induced by SR Ca2+ release.
J Clin Invest. 2021 Apr 1;131(7):e137752
pig cardiomyocytes
100 μmol/L
To investigate the inhibitory effect of Gap19 on Cx43 hemichannels, results showed that Gap19 significantly reduced unitary current activities induced by SR Ca2+ release.
J Clin Invest. 2021 Apr 1;131(7):e137752
mouse cardiomyocytes
100 μmol/L
To investigate the inhibitory effect of Gap19 on Cx43 hemichannels, results showed that Gap19 significantly reduced unitary current activities induced by SR Ca2+ release.
J Clin Invest. 2021 Apr 1;131(7):e137752
neurons
100 μM/mL
12 hours
Gap19 slightly blocked the opening of Cx43Hcs in neurons, but the difference was not significant.
J Neuroinflammation. 2020 Oct 28;17(1):322
microglia
100 μM/mL
12 hours
Gap19 slightly blocked the opening of Cx43Hcs in microglia, but the difference was not significant.
J Neuroinflammation. 2020 Oct 28;17(1):322
astrocytes
100 μM/mL
12 hours
Gap19 significantly inhibited the excessive opening of Cx43Hcs in astrocytes after hemin stimulation and reduced GFAP fluorescence intensity, indicating inhibition of astrocyte activation.
Significantly inhibited γ-H2AX-positive cell counts in the bystander zone
Cell Death Dis. 2020 Mar 18;11(3):194
RBE4 cells
200 μM
30 min pretreatment + 3h post-irradiation
Significantly inhibited γ-H2AX-positive cell counts in both irradiated and bystander zones
Cell Death Dis. 2020 Mar 18;11(3):194
ARPE-19 cells
5, 10, 20 μM
1 hour or 24 hours
To assess the impact of XG19 on metabolic activity and cell survival. MTT assays revealed no significant difference in viability between XG19-treated and untreated groups at 1 or 24 hours, indicating no cytotoxicity from XG19 uptake or prolonged presence.
Drug Deliv Transl Res. 2020 Jun;10(3):751-765
human retinal microvascular endothelial cells (hRMEC)
5, 10, 20, 50, 100 μM
1 hour
To evaluate the cellular uptake efficiency of Xentry-Gap19 (XG19) compared to native Gap19 under normal conditions. Results showed that XG19 significantly enhanced uptake at low concentrations (10-20 μM), whereas native Gap19 was barely detectable below 50 μM (hRMEC) or 100 μM (ARPE-19).
Drug Deliv Transl Res. 2020 Jun;10(3):751-765
Gap19 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
Intracerebral hemorrhage model
Intraperitoneal injection
25 mg/kg
Once daily for 3 consecutive days
Gap19 significantly alleviated hematoma volume and neurological deficits after ICH injury, reduced astrocyte activation and proinflammatory cytokine release.
J Neuroinflammation. 2020 Oct 28;17(1):322
Mice
MPTP-induced Parkinsonian model
Intraperitoneal injection
23 mg/kg
4 injections at 2 h intervals, then once daily for 2 days
TAT-Gap19 peptide completely reverted both DN loss and microglial activation in MPTP-injected GRCx30CreERT2 mutant mice; in wild-type mice there was partial but significant survival effect.
Cell Death Differ. 2019 Mar;26(3):580-596
Mice
Permanent middle cerebral artery occlusion (pMCAO) model
Intraperitoneal injection
0.75 μmol/kg or 7.5 μmol/kg
Single dose, evaluated after 2 hours
Evaluate the neuroprotective effect of Gap19 in ischemic stroke, showing significant reduction in infarct volume
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