Fenvalerate-d5 是 Fenvalerate 的氘代物。Fenvalerate 是一种有效的蛋白磷酸酶 2B (钙调神经磷酸酶；calcineurin) 抑制剂，对 PP2B-Aα 的IC50 为 2-4 nM。Fenvalerate 是拟除虫菊酯杀虫剂和杀螨剂。
Fenvalerate-d5 is the deuterium labeled Fenvalerate. Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide[1].
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]. E Enan, et al. Specific Inhibition of Calcineurin by Type II Synthetic Pyrethroid Insecticides. Biochem Pharmacol. 1992 Apr 15;43(8):1777-84.;A R Reilein, et al. Regulation of Organelle Movement in Melanophores by Protein Kinase A (PKA), Protein Kinase C (PKC), and Protein Phosphatase 2A (PP2A). J Cell Biol. 1998 Aug 10;142(3):803-13.
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