Thiorphan (Synonyms: DL-Thiorphan) |
| Catalog No.GC16764 |
Thiorphan is a selective Neprilysin (NEP) inhibitor with an IC50 value of 6.9nM. Thiorphan has antidiarrhoeal and neuroprotective effects.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 76721-89-6
Sample solution is provided at 25 µL, 10mM.
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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.
| Cell experiment [1]: | |
Cell lines | Guinea pig Clara cells |
Preparation Method | Guinea pig Clara cells were treated with Thiorphan (1mM) for 1-2h . |
Reaction Conditions | 1mM; 1-2h |
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]: | |
Animal models | Diabetes model |
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. |
Dosage form | 0.1mg/kg; po; 4 weeks |
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. |
References: | |
| Cas No. | 76721-89-6 | 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 |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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