Thiorphan
(Synonyms: 3-巯基-2苄基丙基甘氨酸,DL-Thiorphan) 目录号 : GC16764
Thiorphan是一种选择性脑啡肽（NEP）抑制剂，IC50值为6.9nM。Thiorphan具有止泻和神经保护作用。
Cas No.:76721-89-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Guinea pig Clara cells |
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Preparation Method |
Guinea pig Clara cells were treated with Thiorphan (1mM) for 1-2h . |
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Reaction Conditions |
1mM; 1-2h |
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Applications |
Treatment of Clara cells with Thiorphan (1mM), an inhibitor of neutral endopeptidase, decreased by 44 and 26% the levels of immunoreactive endothelin (ir-ET) in the cell supernatant respectively, after 1 and 2h incubation periods. |
| Animal experiment [2]: | |
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Animal models |
Diabetes model |
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Preparation Method |
Diabetes was induced by administration of Streptozotocin (55mg/kg, ip) in male Wistar rats. After 4 weeks, diabetic rats were subjected to either Thiorphan (0.1mg/kg/day, po) or Telmisartan (10mg/kg/day, po) monotherapy, or their combination, for a period of 4 weeks. |
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Dosage form |
0.1mg/kg; po; 4 weeks |
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Applications |
Monotherapy with Thiorphan or Telmisartan reduced levels of PGL, CK-MB, and LDH to a certain extent, but the combination regimen additively improved metabolic perturbations in DC rats. |
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References: |
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Thiorphan is a selective Neprilysin (NEP) inhibitor with an IC50 value of 6.9nM[1]. Thiorphan has antidiarrhoeal and neuroprotective effects[2][3].
The highest non-cytotoxic concentration of Thiorphan (500μM) enhanced the antiproliferative effect of osteosarcoma HOS cells and had a synergistic effect when used in combination with Alpha-ketoglutarate [4]. Thiorphan (10µM; 48h) decreased the OGR1-induced inhibition of A549 cell migration[5].
Thiorphan (50mg/kg) reduced Ibotenate-induced cortical lesions by to 57% and cortical caspase-3 cleavage by to 59%. This neuroprotective effect was long-lasting and was still observed when Thiorphan was administered 12h after the insult[3]. In a rat model of diabetic cardiomyopathy, the combination of Thiorphan (0.1mg/kg/d; po; 4 weeks) and Telmisartan attenuated inflammatory (NF-jB/MCP-1), profibrotic (TGF-b/Smad7), and apoptotic (PARP/Caspase-3) responses[6].
References:
[1].Roques B P, Fournie-Zaluski M C, Soroca E, et al. The enkephalinase inhibitor thiorphan shows antinociceptive activity in mice[J]. Nature, 1980, 288(5788): 286-288.
[2]. Stanović S, Boranić M, Petrovecki M, et al. Thiorphan, an inhibitor of neutral endopeptidase/enkephalinase (CD10/CALLA) enhances cell proliferation in bone marrow cultures of patients with acute leukemia in remission[J]. Haematologia, 2000, 30(1): 1-10.
[3].Medja F, Lelievre V, Fontaine R H, et al. Thiorphan, a neutral endopeptidase inhibitor used for diarrhoea, is neuroprotective in newborn mice[J]. Brain, 2006, 129(12): 3209-3223.
[4]. Mizerska-Kowalska M, Sławińska-Brych A, Niedziela E, et al. Alpha Ketoglutarate Downregulates the Neutral Endopeptidase and Enhances the Growth Inhibitory Activity of Thiorphan in Highly Aggressive Osteosarcoma Cells[J]. Molecules, 2022, 28(1): 97.
[5].Sharma A L, Meitei P M, Machathoibi T C, et al. Ovarian cancer G protein-coupled receptor 1 inhibits A549 cells migration through casein kinase 2α intronless gene and neutral endopeptidase[J]. BMC cancer, 2022, 22(1): 143.
[6]. Malek V, Gaikwad A B. Telmisartan and thiorphan combination treatment attenuates fibrosis and apoptosis in preventing diabetic cardiomyopathy[J]. Cardiovascular Research, 2019, 115(2): 373-384.
Thiorphan是一种选择性脑啡肽（NEP）抑制剂，IC50值为6.9nM[1]。Thiorphan 具有止泻和神经保护作用[2][3]。
Thiorphan的最高无细胞毒性浓度（500μM）增强了骨肉瘤HOS细胞的抗增殖作用，与α-酮戊二酸（Alpha-Ketoglutarate）联合使用时具有协同作用[4]。Thiorphan（10µM；48h）降低了OGR1诱导的A549细胞迁移抑制[5]。
Thiorphan（50mg/kg）可使伊博替尼（Ibotenate）诱发的皮质损伤减少57%，半胱天冬酶-3（caspase-3）裂解减少59%，这种神经保护作用持久，在损伤后12小时服用仍可观察到[3]。在糖尿病性心肌病大鼠模型中，Thiorphan（0.1 mg/kg/d；po；4 weeks）和替米沙坦（Telmisartan）的组合可减弱炎症（NF-JB/MCP-1）、促纤维化（TGF-b/Smad7）和凋亡（PARP/Caspase-3）反应[6]。
| 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 | |||
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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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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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