Ganglioside GT1b is a trisialoganglioside that is characterized by having two sialic residues linked to the inner galactose unit. It binds to the neurotoxins botulinum toxin serotype A (BTxA), BTxA heavy chain, and tetanus toxin with IC50 values of 11, 0.74, and 7.2 μM, respectively.[1] Ganglioside GT1b-containing liposomes bind to the major coat protein VP1 from Merkel cell polyomavirus (MCPyV), which has been identified in Merkel cell carcinomas, identifying ganglioside GT1b as a putative MCPyV receptor. [2] Ganglioside GT1b decreases production of IL-6, IL-10, IgG, IgM, and IgA in human peripheral blood mononuclear cells (PBMCs) by 31.4, 30.5, 60, 59.5, and 58%, respectively, when used at a concentration of 10 μM [3] . Ganglioside GT1b mixture contains ganglioside GT1b molecular species with C18:1 and C20:1 sphingoid backbones.
GT-1 (LCB10-0200) is a siderophore-linked cephalosporin compound that effectively combats clinical isolates of various bacterial species, including P. aeruginosa, Klebsiella oxytoca, Proteus spp., Serratia marcescens, and Enterobacter aerogenes.
GT-0198 is a novel glycine transporter 2 inhibitor showed activity in a mouse model of neuropathic pain. GT-0198 inhibited the function of glycine transporter 2 (GlyT2) in human GlyT2-expressing HEK293 cells and did not bind various major transporters or receptors of neurotransmitters in a competitive manner. GT-0198 is considered to be a comparatively selective GlyT2 inhibitor. GT-0198 is a structurally novel GlyT2 inhibitor bearing a phenoxymethylbenzamide moiety with in vivo efficacy in behavioral models of neuropathic pain.
Cipralisant is a selective histamine H3 receptor antagonist in vivo, and an agonist in vitro (pKi: 9.9 for histamine H3 receptor; Ki: 0.47 nM for rat histamine H3 receptor). It has the potential for the treatment of attention-deficit hyperactivity disorde
Evatanepag, also known as CP-533536, is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation. CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.