Gap Junction Protein

Larazotide acetate is a synthetic peptide. It functions as a tight junction regulator and reverses leaky junctions to their normally closed state.

Gap 26 is a mimetic peptide corresponding to the residues 63-75 of connexin 43, which is a gap junction blocker.

Carbenoxolone disodium (Duogastrone) salt is an agent derived from licorice root. It is used for the treatment of digestive tract ulcers, especially in the stomach. Antidiuretic side effects are frequent, but otherwise, the drug is low in toxicity.

Carbenoxolone (Biogastrone) is an inhibitor of 11β-HSD and gap junction connexin channels. Carbenoxolone inhibits macrophage migration into atria and prevents the development of fatty liver disease.

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

Gap 27 is a peptide(Ser-Arg-Pro-Thr-Glu-Lys-Thr-Ile-Phe-Ile-Ile) derived from connexin 43 that is a selective gap junction blocker.

Rotigaptide TFA(355151-12-1 free base) is a novel and specific modulator of Cx43 and is a potent AAP. Rotigaptide TFA(355151-12-1 free base) prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress.

Meclofenamic acid sodium (Movens), a non-steroidal anti-inflammatory agent, has properties of antipyretic and antigranulation activities. It also inhibits prostaglandin biosynthesis.

Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and no intrinsic sympathomimetic activity.

Danegaptide Hydrochloride (GAP-134 (Hydrochloride)) (GAP-134 Hydrochloride) is a selective modifier of the gap junction protein.

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.

Tonabersat (SB-220453) is a novel and orally available gap-junction modulator and CSD (Cortical spreading depression) inhibitor that regulates cellular communication between trigeminal ganglion neuronal cells and glial cells and inhibits neurogenic inflammation for the treatment of migraine and epilepsy.

Meclofenamic acid (Meclofenamate) is a non-selective gap-junction blocker and a selective inhibitor of the fat mass and obesity-associated (FTO) enzyme, with notable anti-inflammatory activities.

Meclofenamate sodium is a potent non-steroidal anti-inflammatory agent, which can specifically inhibit chemokine-induced human polymorphonuclear leukocyte function: chemotaxis, degranulation, and superoxide anion free radical production.

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

Rotigaptide is a novel and specific modulator of Cx43 and is a potent AAP. Rotigaptide prevents the uncoupling of Cx43-mediated gap junction communication and normalizes cell-to-cell communication during acute metabolic stress.

Peptide5 TFA, a connexin 43 mimetic peptide, mitigates swelling, astrogliosis, and neuronal cell death in animal models of spinal cord injury, and suppresses the NLRP3 inflammasome, functioning as an anti-inflammatory agent (1) (2) (3).

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

Danegaptide (GAP-134), has been identified as a potent and selective second generation gap junction modifier with oral bioavailability.a small modified dipeptide.

Connexin43 mimetic peptide. Reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal cord injury ex vivo and in vivo. Exhibits analgesic effects in models of neuropathic pain. O'Carroll et al (2008) Connexin 43 mimetic peptides reduce swelling, astrogliosis and neuronal cell death after spinal cord injury. Cell.Commun.Adhes. 15 27 PMID:18649176 |Mao et al (2017) Characterisation of Peptide5 systemic administration for treating traumatic spinal cord injured rats. Exp.Brain.Res. 235 3033 PMID:28725925 |Kim et al (2017) Characterising the mode of action of extracellular Connexin43 channel mimetic peptides in an in vitro ischemia injury model. Biochem.Biophys.Acta. 1861 68 PMID:27816754 |Tonkin et al (2017) Attenuation of mechanical pain hypersensitivity by treatment with Peptide5, a connexin-43 mimetic peptide, involves inhibition of NLRP3 inflammasome in nerve-injured mice. Exp.Neurol. 300 1 PMID:29055716

Osemitamab (FUT8-KO) is a monoclonal antibody targeting claudin-18.2, expressed in CHO cells with a knockout of the fucosyltransferase 8 gene (FUT8). The absence of fucose heightens the antibody's ADCC effect. When combined with Capecitabine and Oxaliplatin, it can be used for G/GEJ cancer research.

Larazotide is an octapeptide paracellular permeability inhibitor whose structure is derived from a protein (zonula occludens toxin) secreted by Vibrio cholerae for treatment of Coeliac disease.

AT-1002 is a tight junction regulator and absorption enhancer. It is a 6-mer synthetic peptide.

PQ1 Succinate, a gap junction enhancer, acts by restoring GJIC and increasing connexin expression in breast cancer cell lines while not affecting normal mammary cells.