Thiorphan (Synonyms: DL-Thiorphan) |
| Catalog No.GC16764 |
Thiorphan은 선택적인 Neprilysin (NEP) 억제제로 IC50 값이 6.9nM이다. Thiorphan은 항설사 및 신경 보호 효과가 있다.
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Cas No.: 76721-89-6
Sample solution is provided at 25 µL, 10mM.
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Thiorphan은 선택적인 Neprilysin (NEP) 억제제로 IC50 값이 6.9nM이다. Thiorphan은 항설사 및 신경 보호 효과가 있다.
Thiorphan의 가장 높은 무세포 독성 농도(500μM)는 골육종 HOS 세포의 항증식 효과를 강화했고 알파-케토글루타르산과 함께 사용할 때 시너지 효과를 나타냈다[4]. Thiorphan (10µM; 48시간)은 OGR1에 의해 유도된 A549 세포 이동 억제를 감소시켰다[5].
Thiorphan（50mg/kg）은 Ibotenate 유발의 피질 손상을 57%나 감소시키고 피질 caspase-3 분리도 59% 감소시켰다. 이 신경 보호 효과는 장기적이고 Thiorphan을 손상 후 12시간에 투여해도 여전히 관찰할 수 있다[3]. 당뇨병성 심근병 모델의 쥐에서 Thiorphan（0.1mg/kg/일; 구강 투여; 4주）와 Telmisartan의 조합은 염증성（NF-κB/MCP-1）、섬유화（TGF-β/Smad7）및 조절사（PARP/Caspase-3）반응을 완화시켰다[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.
| 세포 실험 [1]: | |
세포 라인 | 기니 피그 클라라 세포 |
제조 방법 | 기니 피그 클라라 세포는 Thiorphan（1mM）으로 1-2시간 동안 처리되었습니다. |
반응 조건 | 1mM; 1-2시간 동안 |
응용 분야 | Thiorphan（1mM），중성 내펩타이드 효소 억제제로 클라라 세포에 처리한 결과 1시간과 2시간 발균 기간 후에 세포 상층액에서의 면역반응성 내피렐린(ir-ET) 수준이 각각 44%와 26% 감소했습니다. |
| 동물 실험 [2]: | |
동물 모형 | 당뇨병 모델 |
제조 방법 | 수컷 Wistar 쥐에 Streptozotocin (55mg/kg, ip) 투여로 당뇨병이 유발되었다.4주 후 당뇨 쥐에게 Thiorphan (0.1mg/kg/day, po) 또는 Telmisartan (10mg/kg/day, po) 단독요법 또는 이들의 조합을 4주 동안 실시하였다. |
제형 | 0.1mg/kg; po; 4 주 동안 |
응용 분야 | Thiorphan이나 Telmisartan 단독 치료는 PGL, CK-MB, LDH 수준을 일정 정도로 낮췄지만 조합 치료는 당뇨병성 심장병（DC）쥐의 신진대사 동요를 추가로 개선했습니다. |
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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