الصفحة الرئيسية>>Signaling Pathways>> Proteases>> Carboxypeptidase>>2-Guanidinoethylmercaptosuccinic Acid

2-Guanidinoethylmercaptosuccinic Acid (Synonyms: GEMSA)

رقم الكتالوجGC11804

2-Guanidinoethylmercaptosuccinic Acid (2-Guanidinoethylmercaptosuccinic acid) هو مثبط نوعي قوي لإنزيم المعالجة الشبيه بالكاربوكسي ببتيداز B (encephalin convertase) بقيمة Ki البالغة 8.8 نانومتر.

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2-Guanidinoethylmercaptosuccinic Acid التركيب الكيميائي

Cas No.: 77482-44-1

الحجم السعر المخزون الكميّة
5mg
258٫00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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).

Chemical Properties

Cas No. 77482-44-1 SDF
المرادفات 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
الذوبان Water: Soluble Storage Store at 4°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 4.2499 mL 21.2495 mL 42.4989 mL
5 mM 0.85 mL 4.2499 mL 8.4998 mL
10 mM 0.425 mL 2.1249 mL 4.2499 mL
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