CRS3123 dihydrochloride
Based on 1 publication(s) in Google Scholar
CRS3123 dihydrochloride (REP-3123 dihydrochloride) is an orally active antibacterial agent that targets methionyl-tRNA synthetase (MetRS). CRS3123 dihydrochloride 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 dihydrochloride can be used in research on Clostridioides difficile infection and vancomycin-resistant enterococcal infection.
For research use only. We do not sell to patients.
- Purity : 99.11%
- CAS No.: 1013915-99-5
- Formula: C19H21Br2Cl2N3O2S
- Molecular Weight:586.17
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) CRS3123 dihydrochloride
MoreAll Antibiotic Isoforms
More
Biological Activity
Description
|
MetRS |
In Vitro
CRS3123 dihydrochloride (MIC <0.007-0.031 μg/mL) shows MIC <0.007 μg/mL against most enterococci isolates, including VRE, except E. faecalis HM-335 (0.031 μg/mL)[1].
CRS3123 dihydrochloride (5-10× MIC; 24 h) is bacteriostatic against E. faecium NR-31909[1].
CRS3123 dihydrochloride (10 days) maintains low resistance development in E. faecalis ATCC 29212 and E. faecium NR-31909 over 10 serial passages, with only 4-16-fold MIC increases[1].
CRS3123 dihydrochloride (0.5-1 μg/mL) inhibits C. difficile, including B1/NAP1/027 strains, with an MIC90 of 1 μg/mL[2].
CRS3123 dihydrochloride inhibits C. difficile toxin production[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Vero cells (monkey kidney epithelial cells)
-
Concentration:16 µg/mL (no toxicity); 32 µg/mL (20% cytotoxicity)
-
Incubation Time:24 h; 4 h (MTS/PMS)
-
Result:Demonstrated no toxicity up to 16 µg/mL but exhibited 20% cytotoxicity at 32 µg/mL, indicating mild toxicity at this concentration.
Based on the IC50-to-MIC50 comparison, CRS3123 had a ratio of >4571.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1013915-99-5
-
Appearance Solid
-
Molecular Weight 586.17
-
Formula C19H21Br2Cl2N3O2S
-
Color White to off-white
-
SMILES
O=C1C2=C(C=CS2)NC(NCCCN[C@@H]3CCOC4=C(Br)C=C(Br)C=C34)=C1.[H]Cl.[H]Cl
-
Synonyms
REP-3123 dihydrochloride
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
-
Journal Impact Factor
-
Most Recent
-
Expert Opin Investig Drugs
2025 Nov;34(11):869-885. PMID: 41117146
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (170.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
-
Data Sheet (277 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7060 mL | 8.5299 mL | 17.0599 mL | 42.6497 mL |
| 5 mM | 0.3412 mL | 1.7060 mL | 3.4120 mL | 8.5299 mL | |
| 10 mM | 0.1706 mL | 0.8530 mL | 1.7060 mL | 4.2650 mL | |
| 15 mM | 0.1137 mL | 0.5687 mL | 1.1373 mL | 2.8433 mL | |
| 20 mM | 0.0853 mL | 0.4265 mL | 0.8530 mL | 2.1325 mL | |
| 25 mM | 0.0682 mL | 0.3412 mL | 0.6824 mL | 1.7060 mL | |
| 30 mM | 0.0569 mL | 0.2843 mL | 0.5687 mL | 1.4217 mL | |
| 40 mM | 0.0426 mL | 0.2132 mL | 0.4265 mL | 1.0662 mL | |
| 50 mM | 0.0341 mL | 0.1706 mL | 0.3412 mL | 0.8530 mL | |
| 60 mM | 0.0284 mL | 0.1422 mL | 0.2843 mL | 0.7108 mL | |
| 80 mM | 0.0213 mL | 0.1066 mL | 0.2132 mL | 0.5331 mL | |
| 100 mM | 0.0171 mL | 0.0853 mL | 0.1706 mL | 0.4265 mL |
CRS3123 dihydrochloride Related Classifications
HY-115440 Related Classifications
Powered by Bioz
Keywords
- CRS3123
- 1013915-99-5
- REP-3123
- CRS 3123
- CRS-3123
- REP3123
- REP 3123
- Antibiotic
- Bacterial
- Clostridioides difficile infection
- Enterococcus faecium
- Staphylococcus aureus
- Streptococcus pyogenes
- bacteriostatic
- methionyl-tRNA synthetase
- protein synthesis
- sporulation
- toxin production
- vancomycin-resistant enterococci infection
- Inhibitor
- inhibitor
- inhibit