2-Guanidinoethylmercaptosuccinic Acid |
| Catalog No.: GC11804 |
2-Guanidinoethylmercaptosuccinic Acid (2-Guanidinoethylmercaptosuccinic acid) is a potent specific inhibitor of carboxypeptidase B-like processing enzyme (encephalin convertase) with the Ki value of 8.8 nM.
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ki: 8.8 nM
2-Guanidinoethylmercaptosuccinic acid is a carboxypeptidase E inhibitor.
Carboxypeptidase E, also known as enkephalin convertase, can remove C-terminal residues during the processing of propeptides, such as enkephalin and proinsulin.
In vitro: 2-Guanidinoethylmercaptosuccinic acid was identified as a biproduct analogs of lysine and arginine that showed potent inhibitory effect on enkephalin convertase with the Ki value of 8.8 nM. In addition, 2-guanidinoethylmercaptosuccinic acid was found to be several hundred fold more potent towards enkephalin convertase than towards carboxypeptidase B or N and the kinetic analyses indicated the pure competitive nature of the inhibition [1].
In vivo: Previous study found that following the intrathecal administration of 2-guanidinoethylmercaptosuccinic acid at 12.5, 25 and 50 micrograms, an increase in the tail-flick latency was seen. In addition, 2-guanidinoethylmercaptosuccinic acid could potentiate the analgesic effects of the intrathecally applied Met5-enkephalin-Arg6-Phe7 and Met5-enkephalin-Arg6-Gly7-Leu8. All these effects of 2-guanidinoethylmercaptosuccinic acid were significantly attenuated by the treatment of naloxone. Moreover, the rats subjected to chronic pain showed a weaker analgesic response to the treatment of 2-guanidinoethylmercaptosuccinic acid. Furthermore, 2-guanidinoethylmercaptosuccinic acid bound to enkephalin convertase in the spinal cord of these rats produced only a slight increase in KD [2].
Clinical trial: Up to now, 2-guanidinoethylmercaptosuccinic acid is still in the preclinical development stage.
References:
1. Fricker LD, Plummer TH Jr, Snyder SH. Enkephalin convertase: potent, selective, and irreversible inhibitors. Biochem Biophys Res Commun. 1983 Mar 29;111(3):994-1000.
2. M. Bommer, K. Nikolarakis, E. P. Noble, et al. In vivo modulation of rat hypothalamic opioid peptide content by intracerebroventricular injection of guanidinoethylmercaptosuccinic acid (GEMSA): Possible physiological role of enkephalin convertase. Brain Research 492(1-2), 305-313 (1989).
| Cas No. | 77482-44-1 | SDF | |
| Synonyms | GEMSA | ||
| Chemical Name | 2-[[2-[(aminoiminomethyl)amino]ethyl]thio]-butanedioic acid | ||
| Canonical SMILES | OC(C(CC(O)=O)SCCNC(N)=N)=O | ||
| Formula | C7H13N3O4S | M.Wt | 235.3 |
| Solubility | Water: Soluble | Storage | Store at 4°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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