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品質等級
化驗
≥98% (TLC)
形狀
powder
mp
138 °C
溶解度
ethanol: soluble 49.00-51.00 mg/mL, clear, colorless
SMILES 字串
OC(=O)CNC(=O)C(CS)Cc1ccccc1
InChI
1S/C12H15NO3S/c14-11(15)7-13-12(16)10(8-17)6-9-4-2-1-3-5-9/h1-5,10,17H,6-8H2,(H,13,16)(H,14,15)
InChI 密鑰
LJJKNPQAGWVLDQ-UHFFFAOYSA-N
基因資訊
human ... ACE(1636) , ECE1(1889)
rat ... Ace(24310) , Mme(24590)
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一般說明
Thiorphan,又称DL-巯基-2-苄基丙酰基-甘氨酸,是一种纳摩尔浓度量级的脑啡肽酶特异有效抑制剂。它是中性内肽酶的一种抑制剂,可与骨髓细胞中的分化簇10(CD10)发生相互作用,并可能对造血功能进行调节。Thiorphan是一种用于腹泻的安全药物。它可防止新生小鼠的皮质损伤,也是治疗脑瘫(CP)的一种有效药物。
應用
DL-Thiorphan已被用于评估NEP依赖性中性内肽酶的活性。 DL-Thiorphan也被用于通过荧光检测确定NEP酶的活性。
生化/生理作用
脑啡肤酶抑制剂。
準備報告
DL-Thiorphan可以49.00 - 51.00 mg/ml的浓度溶于乙腈并产生一种透明无色的溶液。
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
個人防護裝備
Eyeshields, Gloves, type N95 (US)
其他客户在看
Thiorphan, a neutral endopeptidase inhibitor used for diarrhoea, is neuroprotective in newborn mice
Brain, 129(12), 3209-3223 (2006)
Methionine enkephalin suppresses metabolic activity of a leukemic cell line (NALM-1) and enhances CD10 expression
International Immunopharmacology, 3, 707-711 (2003)
Global brain delivery of neprilysin gene by intravascular administration of AAV vector in mice
Scientific Reports (2013)
Thiorphan, an inhibitor of neutral endopeptidase/enkephalinase (CD10/CALLA) enhances cell proliferation in bone marrow cultures of patients with acute leukemia in remission
Haematologia, 30(1), 1-10 (2000)
Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 60(3), 393-399 (2018-07-14)
Patients with metastatic medullary thyroid cancer (MTC) have limited systemic treatment options. The use of radiolabeled gastrin analogs targeting the cholecystokinin-2 receptor (CCK2R) is an attractive approach. However, their therapeutic efficacy is presumably decreased by their enzymatic degradation in vivo.
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