6α-Hydroxy Paclitaxel-d5 是 6α-Hydroxy paclitaxel 的氘代物。6α-Hydroxy paclitaxel 是紫杉醇的初级代谢物。6α-Hydroxy paclitaxel 对有机阴离子转运多肽 1B1/SLCO1B1 (OATP1B1) 具有与紫杉醇相似的时间依赖性抑制效力，但它对 OATP1B3 不具有时间依赖性作用。6α-Hydroxy paclitaxel 可用于癌症研究。
6α-Hydroxy Paclitaxel-d5 is the deuterium labeled 6α-Hydroxy paclitaxel. 6α-Hydroxy paclitaxel is a primary metabolite of Paclitaxel. 6α-Hydroxy paclitaxel retains a time-dependent effect on organic anion-transporting polypeptides 1B1/SLCO1B1 (OATP1B1) with similar inhibition potency to Paclitaxel, whereas it no longer showed time-dependent inhibition of OATP1B3. 6α-Hydroxy paclitaxel can be used for the research of cancer[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]. Mori D, et al. Alteration in the Plasma Concentrations of Endogenous Organic Anion-Transporting Polypeptide 1B Biomarkers in Patients with Non-Small Cell Lung Cancer Treated with Paclitaxel. Drug Metab Dispos. 2020 May;48(5):387-394.
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