Tacrolimus-13C,d2(Synonyms: FK506-13C,d2; Fujimycin-13C,d2; FR900506-13C,d2)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Tacrolimus-13C,d2 (Synonyms: FK506-13C,d2; Fujimycin-13C,d2; FR900506-13C,d2)

Tacrolimus-13C,D2 (FK506-13C,D2) 是一种13C 和氘代标记的 Tacrolimus。Tacrolimus (FK506)，大环内酯类，与 FK506 结合蛋白 (FKBP) 结合形成复合物并抑制钙调神经磷酸酶 (calcineurin phosphatase)，从而抑制 T 淋巴细胞信号转导和 IL-2 转录。具有强免疫抑制特性。

Tacrolimus-13C,d2(Synonyms: FK506-13C,d2; Fujimycin-13C,d2; FR900506-13C,d2)

Tacrolimus-13C,d2 Chemical Structure

CAS No. : 1356841-89-8

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生物活性

Tacrolimus-13C,D2 (FK506-13C,D2) is a 13C-labeled and deuterium labeled Tacrolimus. Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties[1].

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

807.02

Formula

C4313CH67D2NO12
CAS 号

1356841-89-8
中文名称

他克莫司 13C,d2
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]. Thomson AW, et al. Mode of action of Tacrolimus (FK506): molecular and cellular mechanisms. Ther Drug Monit. 1995 Dec;17(6):584-91.;Vogel KR, et al. mTOR inhibitors rescue premature lethality and attenuate dysregulation of GABAergic/glutamatergic transcription in murine succinate semialdehyde dehydrogenase deficiency (SSADHD), a disorder of GABA metabolism. J Inherit Metab Dis. 2016 Nov;39(6):877-886.;Zhu H, et al. Tacrolimus promotes hepatocellular carcinoma and enhances CXCR4/SDF 1α expression in vivo. Mol Med Rep. 2014 Aug;10(2):585-92.;Okada Y, et al. Tacrolimus ameliorates dextran sulfate sodium-induced colitis in mice: implication of interleukin-1β suppression. Biol Pharm Bull. 2011;34(12):1823-7.;Yuwei He, et al. Drug targeting through platelet membrane-coated nanoparticles for the treatment of rheumatoid arthritis. Nano Res. 30 June 2018.

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