Raloxifene 6-glucuronide-d4 lithium

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Raloxifene 6-glucuronide-d4 lithium 

Raloxifene 6-glucuronide-d4 (lithium) 是 Raloxifene 6-glucuronide 氘代物。Raloxifene 6-glucuronide 是 Raloxifene 的主要代谢产物。Raloxifene 6-glucuronide 的形成主要由 UGT1A1 和 UGT1A8 介导，以 IC50 为 290 μM 与 estrogen receptor 结合。 Raloxifene 是选择性非甾体雌激素受体调节剂。Raloxifene 在纳摩尔浓度激活 TGFβ3 启动子为完全激动剂，并抑制含雌激素反应元件的卵黄蛋白原启动子的表达。

Raloxifene 6-glucuronide-d4 lithium

Raloxifene 6-glucuronide-d4 lithium Chemical Structure

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生物活性

Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].

体外研究
(In Vitro)

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.
分子量

659.67

Formula

C34H30D4LiNO10S
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

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

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

    [2]. Izgelov D, et al. The Effect of Piperine Pro-Nano Lipospheres on Direct Intestinal Phase II Metabolism: The Raloxifene Paradigm of Enhanced Oral Bioavailability. Mol Pharm. 2018 Apr 2;15(4):1548-1555.

    [3]. Kemp DC, et al. Characterization of raloxifene glucuronidation in vitro: contribution of intestinal metabolism to presystemic clearance. Drug Metab Dispos. 2002 Jun;30(6):694-700.

    [4]. Yang NN, et al. Estrogen and raloxifene stimulate transforming growth factor-beta 3 gene expression in rat bone: a potential mechanism for estrogen- or raloxifene-mediated bone maintenance. Endocrinology. 1996 May;137(5):2075-84.

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