| Size | Price | Stock | Qty |
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| 25mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Tacrolimus (formerly also known as FK-506), a macrocyclic lactone isolated from the culture broth of a strain of Streptomyces tsukubaensis, is an immunosuppressive agent used mainly after allogeneic organ transplant to reduce the activity of the patient's immune system and to lower the risk of organ rejection. It is also used in a topical preparation in the treatment of atopic dermatitis (eczema), severe refractory uveitis after bone marrow transplants, exacerbations of minimal change disease, TH2-mediated diseases such as Kimura's disease, and the skin condition vitiligo. FK-506 has strong immunosuppressive activity in vivo and prevents the activation of T-lymphocytes in response to antigenic or mitogenic stimulation in vitro.
| ln Vitro |
Activation of NO synthase, IL-2 gene transcription, cell degranulation, and apoptosis are among the calcium-dependent processes that are inhibited by tacrolimus monohydrate (FK506 monohydrate, Fujimycin monohydrate, FR900506 monohydrate). By binding to FKBPs inside the hormone receptor complex and inhibiting degradation, tacrolimus also increases the effects of progesterone and glucocorticoids. The drug might increase TGFβ-1 gene expression in a manner similar to what has been seen for CsA. Tacrolimus inhibits T cell growth in response to T cell receptor ligation[1]. The treatment of MH3924A cells with a low dosage of Tacrolimus (FK506, 10 μg/L) does not greatly impact their ability to proliferate (P=0.135). Treatment with increasing concentrations of Tacrolimus (100-1,000 μg/L) dramatically increases (P<0.01) the proliferation of MH3924A cells. AMD3100 treatment, at any dose (10, 50, or 100 μg/L), does not appear to affect the proliferation of MH3924A cells (P>0.05). However, the in vitro proliferation of MH3924A cells is boosted (P<0.01)[3] when different doses of AMD3100 are coupled with 100 μg/L Tacrolimus.
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| ln Vivo |
Mice treated with Dextran sulfate sodium (DSS) from Days 10 to 16 or 23 are given Tacrolimus to study the therapeutic effect on the progression and maintenance of colitis. In comparison to normal animals, the control group treated with DSS exhibited a substantial reduction in colon length and an increase in colon weight at Days 17 and 24. Furthermore, the control group's colon weight per unit length is more than twice as high as the normal group's. While Tacrolimus treatment for 7 or 14 days considerably suppresses increases in colon weight per unit length in rats treated with DSS as compared to the control group, the colon shortening is not actually restored by this treatment. Furthermore, as indicated by the inhibitory percentages (59% vs. 28%), the inhibitory effect of tacrolimus on increases in colon weight per unit length is more pronounced with a 14-d treatment than a 7-d treatment[4].
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| References |
[1]. Thomson AW, et al. Mode of action of Tacrolimus (FK506): molecular and cellular mechanisms. Ther Drug Monit. 1995 Dec;17(6):584-91.
[2]. Okada Y, et al. Tacrolimus ameliorates dextran sulfate sodium-induced colitis in mice: implication of interferon-γ and interleukin-1β suppression. Biol Pharm Bull. 2011;34(12):1823-7. [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 |
| Molecular Formula |
C44H71NO13
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| Molecular Weight |
822.05
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| CAS # |
109581-93-3
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| Related CAS # |
Tacrolimus;104987-11-3
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| SMILES |
CO[C@@H]1C[ C@H](/C=C([ C@H]2OC([C@@H]3CCCCN3C(C([C@@]4(O[C@@H]([C@@H](OC)C[ C@H]4C)[C@@H](OC)C[ C@H](C/C(C)=C/[ C@H](C(C[C@@H]([ C@H]2C)O)=O)CC=C)C)O)=O)=O)=O)\C)CC[ C@H]1O.O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (3.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2165 mL | 6.0824 mL | 12.1647 mL | |
| 5 mM | 0.2433 mL | 1.2165 mL | 2.4329 mL | |
| 10 mM | 0.1216 mL | 0.6082 mL | 1.2165 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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