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2-Guanidinoethylmercaptosuccinic Acid
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
2-Guanidinoethylmercaptosuccinic Acid图片
CAS NO:77482-44-1
包装:5mg
市场价:2674元

产品介绍

化学性质

Physical AppearanceA solid
StorageStore at -20°C
M.Wt235.3
Cas No.77482-44-1
FormulaC7H13N3O4S
SynonymsGEMSA
SolubilitySoluble in DMSO
Chemical Name2-[[2-[(aminoiminomethyl)amino]ethyl]thio]-butanedioic acid
Canonical SMILESOC(C(CC(O)=O)SCCNC(N)=N)=O
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。

资料参考

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).