Thiorphan-d5

Thiorphan-d5 is intended for use as an internal standard for the quantification of thiorphan (Cay-15600) by GC- or LC-MS. 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: (3-mercapto-2-((phenyl-d5)methyl)propanoyl)glycine. CAS Number: 2183240-70-0. Molecular Formula: C12H10D5NO3S. Formula Weight: 258.3. Purity: >99% deuterated forms (d1-d5). Formulation: (Request formulation change), A solid. Solubility: DMSO: soluble, Methanol: soluble. SMILES: O=C(NCC(O)=O)C(CS)CC1=C([2H])C([2H])=C([2H])C([2H])=C1[2H]. 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)/i1D,2D,3D,4D,5D. InChi Key: LJJKNPQAGWVLDQ-RALIUCGRSA-N.