| CAS NO: | 77482-44-1 |
| 包装: | 5mg |
| 市场价: | 2268元 |
| Cas No. | 77482-44-1 |
| 别名 | GEMSA |
| 化学名 | 2-[[2-[(aminoiminomethyl)amino]ethyl]thio]-butanedioic acid |
| Canonical SMILES | OC(C(CC(O)=O)SCCNC(N)=N)=O |
| 分子式 | C7H13N3O4S |
| 分子量 | 235.3 |
| 溶解度 | Water: Soluble |
| 储存条件 | Store at 4℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: |
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