Sograzepide-d3 (Netazepide-d3) is the deuterium labeled Sograzepide. Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC₅₀ value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC₅₀ of 502 nM^[1]. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with K_i values of 0.068, 0.62 and 0.19 nM, respectively^[2].

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

501.59

C₂₈H₂₇D₃N₆O₃

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

  [2]. Boyce M, et al. Effect of netazepide, a gastrin/CCK2 receptor antagonist, on gastric acid secretion and rabeprazole-induced hypergastrinaemia in healthy subjects. Br J Clin Pharmacol. 2015 May;79(5):744-55.

  [3]. Takinami Y, et al. YF476 is a new potent and selective gastrin/cholecystokinin-B receptor antagonist in vitro and in vivo.Aliment Pharmacol Ther. 1997 Feb;11(1):113-20.