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Tacrolimus monohydrate CAS: 109581-93-3

Category: Inhibitors
Product Name: Tacrolimus monohydrate
Cat No: I000405
CAS No: 109581-93-3
Molecular Formula: C44H71NO13
Molecular Weight: 822.03
Solubility: 10 mM in DMSO
IC50: 0.47 nM (Inhibition of lymphocyte proliferation) [1]
CAS 109581-93-3,Tacrolimus monohydrate
  • Description

Tacrolimus monohydrate(FK506; FR900506) is a potent immunosuppressive drug often administered to transplant recipient patients and exhibits a variety of adverse cardiovascular effects.
IC50 Value: 0.47 nM (Inhibition of lymphocyte proliferation) [1]
in vitro: MP and tacrolimus decreased the number of circulating helper-T cells with IC50 values of 23 ng/ml for MP and 6.7 ng/ml for tacrolimus. After coadministration of these drugs, an interaction occurs, but the nature (additive or antagonistic) of this interaction was not clear. The IC50 of tacrolimus for in vitro inhibition of lymphocyte proliferation was 0.39 ng/ml (0.47 nM) and 1.02 ng/ml (2.73 nM) for MP. The maximum percentage of inhibition was 94.6% for tacrolimus and 64.9% for MP [1]. K506 inhibited the proliferation of T cell clones stimulated with specific antigens in a dose-dependent manner, and at about 100-fold lower concentrations than CsA. FK506 inhibited both IL-2 secretion and IL-2 receptor expression of BC.21 after stimulation with the specific antigen. FK506 also inhibited the proliferation of BC.21 stimulated with phorbol 12-myristate 13-acetate plus calcium ionophore [2].
in vivo: Rat kidney TAC concentrations were higher (range 109-190 pg/mg tissue) than those in the liver (range 22-53 pg/mg of tissue), with median tissue/blood concentrations ratios of 72.0 and 17.6, respectively. In 2 transplant patients, kidney TAC concentrations ranged from 119 to 285 pg/mg of tissue and were approximately 20 times higher than whole blood trough TAC concentrations [3].

  • References

[1]. Piekoszewski W, Chow FS, Jusko WJ. Pharmacokinetic and pharmacodynamic effects of coadministration of methylprednisolone and tacrolimus in rabbits. J Pharmacol Exp Ther. 1994 Apr;269(1):103-9.
[2]. Sawada S, Suzuki G, Kawase Y, Novel immunosuppressive agent, FK506. In vitro effects on the cloned T cell activation. J Immunol. 1987 Sep 15;139(6):1797-803.
[3]. Noll BD, Coller JK, Somogyi AA, Validation of an LC-MS/MS Method to Measure Tacrolimus in Rat Kidney and Liver Tissue and Its Application to Human Kidney Biopsies. Ther Drug Monit. 2013 Aug 5.

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