Thiorphan

Thiorphan is an inhibitor of neprilysin (NEP, IC50 = 0.007 µM). 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). Thiorphan (10 µM) increases bradykinin-induced relaxation of isolated porcine coronary artery rings precontracted with potassium chloride under hypoxic, but not normoxic, conditions. Thiorphan reduces increases in gastric acid output induced by pentagastrin (Cay-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. Thiorphan (2 mg/ml, i.c.v.) increases cortical levels of insoluble amyloid-beta (1-40) (Abeta40) and decreases time spent in the platform quadrant in the Morris water maze, indicating impaired reference memory, in rats.Formal Name: N-[2-(mercaptomethyl)-1-oxo-3-phenylpropyl]-glycine. CAS Number: 76721-89-6. Synonyms: DL-Thiorphan. Molecular Formula: C12H15NO3S. Formula Weight: 253.3. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, PBS (pH 7.2): 0.5 mg/ml. SMILES: O=C(NCC(O)=O)C(CS)CC1=CC=CC=C1. InChi Code: 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.