| Thiorphanneprilysin inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity ≥ 95.00%
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Chemical structure
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| Cas No. | 76721-89-6 | SDF | Download SDF |
| Synonyms | DL-Thiorphan | ||
| Chemical Name | N-[2-(mercaptomethyl)-1-oxo-3-phenylpropyl]-glycine | ||
| Canonical SMILES | O=C(NCC(O)=O)C(CS)CC1=CC=CC=C1 | ||
| Formula | C12H15NO3S | M.Wt | 253.3 |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| 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. | ||
Ki: 4-140 nM
Thiorphan is a neprilysin inhibitor.
Neprilysin, also known as membrane metallo-endopeptidase (MME), neutral endopeptidase (NEP), and common acute lymphoblastic leukemia antigen (CALLA) is an enzyme that is encoded by the MME gene. Neprilysin is a zinc-dependent metalloprotease that cleaves peptides at the amino side of hydrophobic residues and inactivates several peptide hormones. Neprilysin also degrades the amyloid beta peptide with abnormal misfolding and aggregation, which has been implicated as a cause of Alzheimer"s disease.
In vitro: A previous study assessed the effect of thiorphan or captopril on proliferation of two human tumor cell lines, A549 and HL60. The results showed that captopril could inhibit the proliferation of both A549 and HL60 cells lines but thiorphan had antiproliferative effect only on A549 cells in a dose-dependent manner. However, neither captopril nor thiorphan treatment in combination with interferon alpha or doxorubicin was able to enhance cytotoxic potential of doxorubicin and cytostatic activity of interferon alpha [1].
In vivo: Animal study found that intraperitoneal administration of thiorphan reduced ibotenate-induced cortical lesions by up to 57% and cortical caspase-3 cleavage by up to 59%. Such neuroprotective effect was long-lasting and was still observed when thiorphan was administered 12 h after the insult, suggesting a remarkable window for therapeutic intervention [2].
Clinical trial: The possibility that the intravenous infusion of acetorphan, a prodrug of thiorphan, can inhibit plasma and cerebrospinal fluid (CSF) enkephalinase in man was investigated. A decrease of approximately 65% in enzyme activity was observed in both plasma and CSF. Acetorphan could not induce any significant variation of plasma angiotensin-converting enzyme activity [3].
References:[1] Kowalski J, Belowski D, Wielgus J, Gabryel B, Klin M, Herman ZS. Effect of captopril and thiorphan on the proliferation of human neoplastic cell lines and their influence on cytostatic activity of interferon alpha or cytotoxic activity of doxorubicin. Arch Immunol Ther Exp (Warsz). 1995;43(1):47-50.[2] Medja F, Lelièvre V, Fontaine RH, Lebas F, Leroux P, Ouimet T, Saria A, Rougeot C, Dournaud P, Gressens P. Thiorphan, a neutral endopeptidase inhibitor used for diarrhoea, is neuroprotective in newborn mice. Brain. 2006 Dec;129(Pt 12):3209-23. [3] Spillantini, M. ,Gepetti, P.,Fanciullacci, M., et al. In vivo “enkephalinase” inhibition by acetorphan in human plasma and CSF. European Journal of Pharmacology 125(1), 147-150 (1986).
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看有关产前诊断的一个资料，提到：“凡是酶活性能在成纤维细胞中表达均可用绒毛或羊水细胞的酶活性测定进行产前诊断，如溶酶体贮积症。”
不太理解，为什么成纤维细胞中表达的酶就能在绒毛或羊水细胞中测出来呢？绒毛的细胞跟成纤维细胞没什么直接关系吧？或者是因为成纤维细胞脱落到羊水中，破裂，然后就可以检测了？
求各位解答，谢谢。
它只是一个检验科的检验设备，用来化验血液、尿液中的成分浓度，医生据此来诊断疾病，可以查很多项目，如乙肝五项等等，不能直接检查什么疾病。
