Eliglustat-d4 (Genz 99067-d4) 是 Eliglustat 的氘代物。Eliglustat是高效特异，有口服活性的葡糖脑苷脂合成酶抑制剂，IC50值为 24 nM。
Eliglustat-d4 (Genz 99067-d4) is the deuterium labeled Eliglustat. Eliglustat is an specific, potent and orally active glucocerebroside synthase inhibitor with an IC50 of 24 nM[1][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].
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. McEachern KA, et al. A specific and potent inhibitor of glucosylceramide synthase for substrate inhibition therapy ofGaucher disease. Mol Genet Metab. 2007 Jul;91(3):259-68.
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