Tacrolimus-d3

Tacrolimus-d3 (FK506-d3) is 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].

Product Specifications

Product Name Alternative

FK506-d3; Fujimycin-d3; FR900506-d3

UNSPSC

12352005

Target

Antibiotic; Autophagy; Bacterial; FKBP; Isotope-Labeled Compounds; Phosphatase

Related Pathways

Anti-infection; Apoptosis; Autophagy; Cell Cycle/DNA Damage; Immunology/Inflammation; Metabolic Enzyme/Protease; Others

Applications

COVID-19-anti-virus

Field of Research

Cancer; Infection; Inflammation/Immunology

Smiles

O=C([C@@](CCCC1)([H])N1C(C([C@@]2(O)[C@H](C)C[C@H](OC)[C@@](O2)([H])[C@@H](OC)C[C@@H](C)C/C(C)=C/C3([2H])CC=C)=O)=O)O[C@H](/C(C)=C/[C@H]4C[C@@H](OC)[C@H](O)CC4)[C@H](C)[C@@H](O)C([2H])([2H])C3=O

Molecular Formula

C44H66D3NO12

Molecular Weight

807.04

References & Citations

[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.|[3]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.|[4]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.|[5]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.|[6]Yuwei He, et al. Drug targeting through platelet membrane-coated nanoparticles for the treatment of rheumatoid arthritis. Nano Res. 30 June 2018.