A NEP inhibitor (IC50 = 0.007 µM); inhibits NEP over NEP2 (IC50 = 22 µM) and ACE and ECE1 (Kis = >100 and >10

Thiorphan – 50 mg

Brand:
Cayman
CAS:
76721-89-6
Storage:
-20
UN-No:
Non-Hazardous - /

Thiorphan is an inhibitor of neprilysin (NEP; IC50 = 0.007 µM).{24072} It selectivity inhibits NEP over NEP2 (IC50 = 22 µM), as well as angiotensin-converting enzyme (ACE) and endothelin-converting enzyme 1 (ECE1; Kis = >0.1 and >10 µM, respectively, in cell-free assays).{24072,25518} Thiorphan (10 µM) increases bradykinin-induced relaxation of isolated porcine coronary artery rings precontracted with potassium chloride under hypoxic, but not normoxic, conditions.{52118} Thiorphan reduces increases in gastric acid output induced by pentagastrin (Item No. 28546) by 64% in rats when administered intracerebroventricularly at a dose of 50 µg, but not when administered intravenously at doses of 1.7 and 17 mg/kg.{52119} Thiorphan (2 mg/ml, i.c.v.) increases cortical levels of insoluble amyloid-β (1-40) (Aβ40) and decreases time spent in the platform quadrant in the Morris water maze, indicating impaired reference memory, in rats.{52120}  

 

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Description

A NEP inhibitor (IC50 = 0.007 µM); inhibits NEP over NEP2 (IC50 = 22 µM) and ACE and ECE1 (Kis = >100 and >10,000 nM, respectively, in cell-free assays); increases bradykinin-induced relaxation of isolated porcine coronary artery rings precontracted with potassium chloride under hypoxic, but not normoxic, conditions at 10 µM; reduces pentagastrin-induced increases in gastric acid output by 64% in rats at 50 µg i.c.v., but not 1.7 and 17 mg/kg i.v.; increases cortical levels of insoluble Aβ40 and decreases time spent in the platform quadrant in the Morris water maze, indicating impaired reference memory, in rats at 2 mg/ml i.c.v.

Formal name: N-[2-(mercaptomethyl)-1-oxo-3-phenylpropyl]-glycine

Synonyms:  DL-Thiorphan

Molecular weight: 253.3

CAS: 76721-89-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases||Research Area|Endocrinology & Metabolism|Carbohydrate Metabolism||Research Area|Endocrinology & Metabolism|Hormones & Receptors||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory||Research Area|Neuroscience|Neurodegenerative Disorders|Alzheimer’s Disease||Research Area|Neuroscience|Neuroendocrinology

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