s-312

Dehydrodeoxy donepezil is an inhibitor of acetylcholinesterase (AChE)

S 312 is a calcium antagonist.

S-312d is a calcium channel antagonist. S-312-d can offer marked neuronal protective effects against ischemic injury.

CRS-3123, a methionyl-tRNA synthetase inhibitor, is used potentially for the treatment of enteric infections.

CRS3123 (REP-3123) dihydrochloride is an orally active, fully synthetic antimicrobial agent that effectively inhibits Clostridioides difficile methionyl-tRNA synthetase (MetRS). CRS3123 dihydrochloride can be used in the study of Clostridioides difficile infection (CDI).

Anti-inflammatory agent 84 (Compound 4D) is a coumarin derivative with notable antibacterial and anti-inflammatory properties. It inhibits E. coli, Candida albicans, Staphylococcus aureus, and methicillin-resistant S. aureus (MRSA) with MIC values of 312, 156, 19, and 316 µg/mL, respectively. Additionally, it suppresses biofilm formation of S. aureus, E. coli, and MRSA, with IC50 values of 185, 321, and 99 µM, respectively. Anti-inflammatory agent 84 also reduces nitric oxide production in lipopolysaccharide-stimulated RAW264.7 macrophages.

PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide production and degranulation in isolated human eosinophils when used at a concentration of 500 μM.3PAR2 (1-6) amide (5 μmol/kg) induces tear secretion in rats when used in combination with amastatin .4 1.Bohm, S.K., Kong, W., Bromme, D., et al.Molecular cloning, expression and potential functions of the human proteinase-activated receptor-2Biochem. J.314(Pt 3)1009-1016(1996) 2.Kanke, T., Ishiwata, H., Kabeya, M., et al.Binding of a highly potent protease-activated receptor-2 (PAR2) activating peptide, [3H]2-furoyl-LIGRL-NH2, to human PAR2Br. J. Pharmacol.145(2)255-263(2005) 3.Miike, S., McWilliam, A.S., and Kita, H.Trypsin induces activation and inflammatory mediator release from human eosinophils through protease-activated receptor-2J. Immunol.167(11)6615-6622(2001) 4.Nishikawa, H., Kawai, K., Tanaka, M., et al.Protease-activated receptor-2 (PAR-2)-related peptides induce tear secretion in rats: Involvement of PAR-2 and non-PAR-2 mechanismsJ. Pharmacol. Exp. Ther.312(2)324-331(2005)