Gap Junction Protein Inhibitor

Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation. Carbenoxolone disodium inhibits Vaccinia virus replication.

Gap 27, a synthetic connexin43 mimetic peptide, is a gap junction inhibitor. Gap 27 possesses conserved sequence homology to a portion of the second extracellular loop leading into the fourth transmembrane connexin segment.

Meclofenamic acid (Meclofenamate) sodium is a non-steroidal anti-inflammatory agent (NSAID). Meclofenamic acid sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat - and obesity-related enzyme (FTO). Meclofenamic acid sodium has anti-inflammatory and antitumor activities.

10Panx is a competitive inhibitor of selective Pannexin 1 (PANX1) channels. 10Panx blocks the opening of PANX1 channels, inhibits ATP release and downstream P2X7 receptor-mediated signaling pathways, thereby reducing cell death and inflammatory responses. 10Panx can be used in the study of diseases such as neuropathic pain, inflammatory bowel disease, and Clostridioides difficile infection. 10Panx can effectively reduce mechanical hyperalgesia and enhanced C-reflexes, and inhibit the expression of pro-inflammatory factors such as IL-6[1][2][3].

Gap 26 is a connexin mimetic peptide, composed of residue numbers 63-75 of the first extracellular loop of connexin 43 (gap junction blocker), containing the SHVR amino acid motif.

ALMB-0168 is a Cx43 hemichannel agonist monoclonal antibody. ALMB-0168 activates Cx43 hemichannels to inhibit the growth and migration of osteosarcoma. ALMB-0168 is applicable to relevant research on osteosarcoma.

Meclofenamic acid (Meclofenamate) is a non-steroidal anti-inflammatory agent. Meclofenamic acid is a highly selective FTO (fat mass and obesity-associated) enzyme inhibitor. Meclofenamic acid competes with FTO binding for the m(6)A-containing nucleic acid. Meclofenamic acid is a non-selective gap-junction blocker. Meclofenamic acid inhibits hKv2.1 and hKv1.1, with IC₅₀ values of 56.0 and 155.9 μM, respectively.

Larazotide acetate is a peptide which is an orally active zonulin antagonist. Larazotide acetate shows antiviral activity to varicella-zoster virus (VZV) with EC₅₀s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide acetate can be used for the research of celiac disease and infection.

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.

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.

Osemitamab is an IgG1 antibody targeting to human claudin-18.2. Osemitamab consists of human-Mus musculus monoclonal TST001 γ1-chain, disulfide with human-Mus musculus monoclonal TST001 κ-chain, dimer (ACI). Osemitamab in combination with Capecitabine (HY-B0016) and Oxaliplatin (HY-17371), can be used for G/GEJ cancer study.

Carbenoxolone is a blood-brain barrier-permeable Pannexin1 inhibitor, gap junction (Gap junction) blocker, and β-amyloid 42 inhibitor. Carbenoxolone modulates voltage-gated currents of wild-type and mutant Panx1, and inhibits stimulus-activated Panx1 channel function. Carbenoxolone interacts with stable residues of β-amyloid 42 peptides, fibrils and oligomers, thereby inhibiting their aggregation. Carbenoxolone alleviates liver fibrosis. Carbenoxolone exerts neuroprotective and nootropic effects. Carbenoxolone can be used in studies related to Alzheimer's disease and liver fibrosis.

Hydroxyflutamide (HFT) is the active metabolite of Flutamide (HY-B0022) and exhibits oral activity. Hydroxyflutamide is a potent androgen receptor antagonist with an IC₅₀ of 700 nM. Hydroxyflutamide can affect embryonic development and reproductive tract development in mice. Additionally, Hydroxyflutamide can enhance the efficacy of Bacillus Calmette-Guérin (BCG) to better inhibit the progression of bladder cancer. Hydroxyflutamide can be used in research related to tumors and reproductive diseases.

EG-2184 is a Pannexin-1 channel inhibitor. EG-2184 can be used in opioid withdrawal related research.

Peptide5, a connexin 43 mimetic peptide, reduce animals swelling, astrogliosis, and neuronal cell death after spinal cord injury

Larazotideis a peptide which is an orally active zonulin antagonist. Larazotide shows antiviral activity to varicella-zoster virus (VZV) with EC₅₀s of 44.14 and 59.06 μM for strain OKA and 07-1, respectively. Larazotide can be used for the research of celiac disease and infection.

Gap 26 TFA is a connexin mimetic peptide, composed of residue numbers 63-75 of the first extracellular loop of connexin 43 (gap junction blocker), containing the SHVR amino acid motif.

Cx43 HC-IN-1 (Compound D4) is a selective and orally active inhibitor of connexin hemichannels (Cx43 HC). Cx43 HC-IN-1 effectively inhibits the hemichannel activity mediated by Cx43/Cx45 in denervated skeletal muscle fibers, significantly increasing the reinnervation rate of muscle fibers by neurons. Cx43 HC-IN-1 reduces neuroinflammation and neuronal overexcitation by inhibiting hemichannels in glial cells in the brain, and alleviates epilepsy in mice. Cx43 HC-IN-1 can be used for research on epilepsy and muscle diseases.

Connexin mimetic peptide 40GAP27 is a biological active peptide. (This peptide corresponds to the GAP27 domain of the second extracellular loop of dominant vascular connexin (Cx40), designated as 40Gap 27. It was used to investigate mechanisms through which oxidant stress impairs communication via gap junctions. When administered, 40Gap27attenuates endothelium-dependent subintimal smooth muscle hyperpolarization.)

Peptide5 TFA, a connexin 43 mimetic peptide, reduces animals swelling, astrogliosis, and neuronal cell death after spinal cord injury. Peptide5 TFA also inhibits NLRP3 inflammasome, and is an anti-inflammatory agent.