77482-44-1 2-Guanidinoethylmercaptosuccinic Acid 羧肽酶E抑制剂 货号C3265
2-Guanidinoethylmercaptosuccinic Acid 羧肽酶E抑制剂 化学性质
CAS号 |
77482-44-1 |
SDF |
Download SDF |
别名 |
GEMSA |
化学名 |
2-[[2-[(aminoiminomethyl)amino]ethyl]thio]-butanedioic acid |
SMILES |
OC(C(CC(O)=O)SCCNC(N)=N)=O |
分子式 |
C7H13N3O4S |
分子量 |
235.3 |
溶解性 |
Soluble in DMSO |
储存条件 |
Store at 4°C |
运输条件 |
试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。 |
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。 |
2-Guanidinoethylmercaptosuccinic Acid 羧肽酶E抑制剂 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.
2-Guanidinoethylmercaptosuccinic Acid 羧肽酶E抑制剂 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).
2-Guanidinoethylmercaptosuccinic Acid 羧肽酶E抑制剂
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