T6031
DL-噻吩
≥98% (TLC), Enkephalinase inhibitor., powder
别名:
(±)-N-(3-巯基-2-苄基丙酰基)甘氨酸, DL-3-巯基-2-苄基丙酰基甘氨酸
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关于此项目
经验公式（希尔记法）:
C12H15NO3S
化学文摘社编号:
分子量:
253.32
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Beilstein/REAXYS Number:
4872101
产品名称
DL-噻吩, ≥98% (TLC)
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)
SMILES string
OC(=O)CNC(=O)C(CS)Cc1ccccc1
InChI key
LJJKNPQAGWVLDQ-UHFFFAOYSA-N
assay
≥98% (TLC)
form
powder
mp
138 °C
solubility
ethanol: soluble 49.00-51.00 mg/mL, clear, colorless
Quality Level
Gene Information
human ... ACE(1636), ECE1(1889)
rat ... Ace(24310), Mme(24590)
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相关类别
General description
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。
Application
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。
Biochem/physiol Actions
脑啡肤酶抑制剂。
Preparation Note
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
Global brain delivery of neprilysin gene by intravascular administration of AAV vector in mice
Iwate N, et al.
Scientific Reports (2013)
Alexander W Sauter et al.
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.
Methionine enkephalin suppresses metabolic activity of a leukemic cell line (NALM-1) and enhances CD10 expression
Martin-Kleiner I, et al.
International Immunopharmacology, 3, 707-711 (2003)
Thiorphan, a neutral endopeptidase inhibitor used for diarrhoea, is neuroprotective in newborn mice
Medja F, et al.
Brain, 129(12), 3209-3223 (2006)
The enkephalinase inhibitor thiorphan shows antinociceptive activity in mice
Roques BP, et al.
Nature, 288(5788), 286-288 (1980)
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