Cayman Thiorphan-d5

Thiorphan-d₅ is intended for use as an internal standard for the quantification of thiorphan (Item No. ) 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; K_is = >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 (Item No. ) 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-β (1-40) (Aβ40) and decreases time spent in the platform quadrant in the Morris water maze, indicating impaired reference memory, in rats.

WARNING This product is not for human or veterinary use.