Thiorphan
(Synonyms: 3-巯基-2苄基丙基甘氨酸,DL-Thiorphan) 目录号 : GC16764A neprilysin inhibitor
Cas No.:76721-89-6
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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).
Cas No. | 76721-89-6 | SDF | |
别名 | 3-巯基-2苄基丙基甘氨酸,DL-Thiorphan | ||
化学名 | N-[2-(mercaptomethyl)-1-oxo-3-phenylpropyl]-glycine | ||
Canonical SMILES | O=C(NCC(O)=O)C(CS)CC1=CC=CC=C1 | ||
分子式 | C12H15NO3S | 分子量 | 253.3 |
溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.9479 mL | 19.7394 mL | 39.4789 mL |
5 mM | 0.7896 mL | 3.9479 mL | 7.8958 mL |
10 mM | 0.3948 mL | 1.9739 mL | 3.9479 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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