1013915-71-3
Chemical Structure
CRS3123
Synonym(s): REP-3123
- CAS No.: 1013915-71-3
- Formula:C19H19Br2N3O2S
- Molecular Weight:513.25
IUPAC Name: (R)-5-((3-((6,8-dibromochroman-4-yl)amino)propyl)amino)thieno[3,2-b]pyridin-7(4H)-one
InChIKey: NNTYBKTXMKBRFA-CQSZACIVSA-N
SMILES: BrC1=C(OCC2)C([C@@H]2NCCCNC3=CC(C(SC=C4)=C4N3)=O)=CC(Br)=C1
Biological Activity: CRS3123 (REP-3123) is an orally active antibacterial agent that targets methionyl-tRNA synthetase (MetRS). CRS3123 competitively displaces methionine from the active site of MetRS, preventing tRNA charging and protein synthesis, and exhibits greater selectivity for C. difficile MetRS than for human MetRS and Gram-negative bacterial MetRS. CRS3123 can be used in research on Clostridioides difficile infection and vancomycin-resistant enterococcal infection[1][2][3][4][5].
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CRS3123 | 99.37% | CRS3123 (REP-3123) is an orally active antibacterial agent that targets methionyl-tRNA synthetase (MetRS). CRS3123 competitively displaces methionine from the active site of MetRS, preventing tRNA charging and protein synthesis, and exhibits greater selectivity for C. difficile MetRS than for human MetRS and Gram-negative bacterial MetRS. CRS3123 can be used in research on Clostridioides difficile infection and vancomycin-resistant enterococcal infection. | ||||||||||||||||||||
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References
- [1]. Abdelmegeed SM, et al. Repurposing antibacterial drugs identifies ridinilazole and CRS3123 as promising candidates against vancomycin-resistant enterococci. Scientific reports. 2025 Dec 18;16(1):264. [Content Brief]
- [2]. Tran MC, et al. New investigational agents for the treatment of Clostridioides difficile infections. Expert Opinion on Investigational Drugs. 2025 Nov 2;34(11):869-85.
- [3]. Nayak SU, et al. Safety, Tolerability, Systemic Exposure, and Metabolism of CRS3123, a Methionyl-tRNA Synthetase Inhibitor Developed for Treatment of Clostridium difficile, in a Phase 1 Study. Antimicrobial agents and chemotherapy. 2017 Aug;61(8):e02760-16.
- [4]. Torrie LS, et al. Discovery of an Allosteric Binding Site in Kinetoplastid Methionyl-tRNA Synthetase. ACS infectious diseases. 2020 May 08;6(5):1044-1057.
- [5]. Louie T, et al. Safety and efficacy of CRS3123 in adults with a primary episode or first recurrence of Clostridioides difficile infection: a phase 2, randomised, double-blind, multicentre, vancomycin-controlled study. The Lancet. Infectious diseases. 2026 May;26(5):535-548.
