| Thiorphanneprilysin inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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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。
如癌症的CA抗原系列、用于测胆汁酸、尿酸之类的酶。
转换酶中的一类。催化氨基酸和a-氧代酸（a-酮酸
)或醛酸之间的氨基转换反应，生成与原来的a-氧代酸或醛酸相应的a-氨基酸或ω-
氨基酸，原来氨基酸转变成相应的氧代酸。转氨酶催化的反应都是可逆的。转氨酶可按底物的不同分成3大类。L-a-氨基酸（酮酸转氨酶） 、ω-
氨基酸（酮酸转氨酶）和D-氨基酸转氨酶。转氨酶的辅基是磷酸吡哆醛或磷酸吡哆胺，两者在转氨基反应中可互相变换。
转氨酶参与氨基酸的分解和合成。氨基酸转氨后生成的酮酸或醛酸可经氧化分解而供能，也可转变成糖类或脂肪酸。相反，酮酸或醛酸也可经转氨酶的作用而生成非必需氨基酸。某些氨基酸之间的互变也有转氨酶参与。在高等动物各组织中，活力最高的转氨酶是谷氨酸
： 草酰乙酸转氨酶（ GOT ）和谷氨酸：丙酮酸转氨酶（GPT）。
转氨酶是人体代谢过程中必不可少的“催化剂”，主要存在于肝细胞内。当肝细胞发生炎症、坏死、中毒等，造成肝细胞受损时，转氨酶便会释放到血液里，使血清转氨酶升高。
通常，体检中主要检查的转氨酶有丙氨酸转氨酶（ALT，俗称谷丙转氨酶）和天门冬氨酸转氨酶（AST，俗称谷草转氨酶），其中尤以前者（ALT）最为常用。1%的肝脏细胞损害，可以使血中ALT的浓度增加1倍。因此，ALT水平可以比较敏感地监测到肝脏是否受到损害。
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