추천 제품
Quality Level
분석
≥98% (TLC)
양식
powder
mp
138 °C
solubility
ethanol: soluble 49.00-51.00 mg/mL, clear, colorless
SMILES string
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 key
LJJKNPQAGWVLDQ-UHFFFAOYSA-N
유전자 정보
human ... ACE(1636) , ECE1(1889)
rat ... Ace(24310) , Mme(24590)
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일반 설명
Thiorphan, also called DL-mercapto-2-benzylpropanoyl-glycine is a specific and potent inhibitor of enkephalinase in nanomolar concentrations. It is an inhibitor of neutral endopeptidase. It interacts with cluster of differentiation 10 (CD10) in bone marrow cells and may modulate hematopoiesis. Thiorphan is a safe drugprescribed for diarrhea. It prevents cortical damage in newborn mice and is a potent agent for treating cerebral palsy.(CP)
애플리케이션
DL-Thiorphan has been used to evaluate the activity of NEP-dependent neutral endopeptidase. DL-Thiorphan has also been used for determining NEP enzymatic activity using fluorimetric assays.
생화학적/생리학적 작용
Enkephalinase inhibitor.
특징 및 장점
This compound is featured on the Neuropeptidases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
제조 메모
DL-Thiorphan is soluble in ethanol at 49.00 - 51.00 mg/ml and yields a clear, colorless solution.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
개인 보호 장비
Eyeshields, Gloves, type N95 (US)
이미 열람한 고객
The enkephalinase inhibitor thiorphan shows antinociceptive activity in mice
Roques BP, et al.
Nature, 288(5788), 286-288 (1980)
Thiorphan, a neutral endopeptidase inhibitor used for diarrhoea, is neuroprotective in newborn mice
Medja F, et al.
Brain, 129(12), 3209-3223 (2006)
Global brain delivery of neprilysin gene by intravascular administration of AAV vector in mice
Iwate N, et al.
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
Stanovic S, et al.
Haematologia, 30(1), 1-10 (2000)
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.
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