Cat. No.: HY-13756A

Tacrolimus monohydrate

(Synonyms: FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate)

105 Cited Publications

Customer Review

Based on 105 publication(s) in Google Scholar

Tacrolimus (FK506) monohydrate, a molecular glue, a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus monohydrate inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties.

For research use only. We do not sell to patients.

Purity: 99.93%
CAS No.: 109581-93-3
Formula: C₄₄H₇₁NO₁₃
Molecular Weight:822.03

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Tacrolimus monohydrate Chemical Structure

CAS No.: 109581-93-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (105)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Macrolide

All Antibiotic Isoforms :

In Vitro

Tacrolimus (FK506) monohydrate inhibits calcium-dependent events, such as IL-2 gene transcription, NO synthase activation, cell degranulation, and apoptosis. Tacrolimus monohydrate also potentiates the actions of glucocorticoids and progesterone by binding to FKBPs contained within the hormone receptor complex, preventing degradation. The agent may enhance expression of the TGFβ-1 gene in a fashion analogous to that demonstrated for CsA. T cell proliferation in response to ligation of the T cell receptor is inhibited by Tacrolimus^[1]. Treatment with a low concentration of Tacrolimus (FK506,10 μg/L) monohydrate does not significantly affect the proliferation of MH3924A cells. Upon treatment with higher concentrations of Tacrolimus (100-1,000 μg/L) monohydrate, the proliferation of MH3924A cells is significantly enhanced (P<0.01). Treatment with AMD3100 at any concentration (10, 50 or 100 μg/L) monohydrate, has no obvious effect on MH3924A cell proliferation (P>0.05). However, when different concentrations of AMD3100 are combined with 100 μg/L Tacrolimus monohydrate, the in vitro proliferation of MH3924A cells is increased (P<0.01)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The therapeutic effect of Tacrolimus monohydrate is investigated on progression and perpetuation of colitis by administering Tacrolimus monohydrate to Dextran sulfate sodium (DSS)-treated mice from Days 10 to 16 or to 23. At Days 17 and 24, colon length is significantly shortened, and colon weight is significantly higher in DSS-treated control animals than in normal animals. In addition, colon weight per unit length in the control group is more than twice that in the normal group. While both 7 and 14 d treatment with Tacrolimus monohydrate significantly suppresses increases in colon weight per unit length in DSS-treated animals compared with the control group, this treatment does not actually restore the colon shortening. In addition, this inhibitory effect of Tacrolimus on increases in colon weight per unit length is more pronounced with 14-d than 7-d treatment, as shown by the inhibitory percentages (59% vs. 28%)^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 109581-93-3
Appearance Solid
Molecular Weight 822.03
Formula C₄₄H₇₁NO₁₃
Color White to yellow
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/[C@H]3CC=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)CC3=O.O
Synonyms

FK506 monohydrate; Fujimycin monohydrate; FR900506 monohydrate
Structure Classification
- Antibiotics
- Macrolide Antibiotics
Initial Source
- Microorganisms
Streptomyces tsukubaensis
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (105)

All IFELISAFlow CytometryWB

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Journal Impact Factor

Signal Transduct Target Ther

Immunity-and-matrix-regulatory cells enhance cartilage regeneration for meniscus injuries: a phase I dose-escalation trial. [Abstract]

2023 Nov 1;8(1):417. PMID: 37907503
Mater Today

2026 Apr 7;96:103326.
Adv Funct Mater

2023 Sep 15.
J Extracell Vesicles

Exosomal PD-L1 functions as an immunosuppressant to promote wound healing. [Abstract]

2019 Dec 27;9(1):1709262. PMID: 33133428

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: J Extracell Vesicles. 2019 Dec 27;9(1):1709262. [Abstract]

Exosomal PD-L1 suppressed T cell activation and promoted skin cell migration in vitro (a). Representative confocal image show the appearance of exosomes as small-red dots. (b-c). Representative confocal images of pre-stained exosomes (red) colocalized with cell membrane (green) of HEK 293T (b) and Jurkat T cells (c).
Exp Hematol Oncol

Effects of molecularly targeted therapies on murine thymus: highly selective mTOR inhibitors induce reversible thymic involution. [Abstract]

2016 Jul 29:5:22. PMID: 27478685
Theranostics

Piezo1-mediated mechanosensation in bone marrow macrophages promotes vascular niche regeneration after irradiation injury. [Abstract]

2022 Jan 16;12(4):1621-1638. PMID: 35198061
Theranostics

FGF19/SOCE/NFATc2 signaling circuit facilitates the self-renewal of liver cancer stem cells. [Abstract]

2021 Mar 5;11(10):5045-5060. PMID: 33754043
Theranostics

STIM1 is a metabolic checkpoint regulating the invasion and metastasis of hepatocellular carcinoma. [Abstract]

2020 May 16;10(14):6483-6499. PMID: 32483465
Theranostics

Sustained Release of Immunosuppressant by Nanoparticle-anchoring Hydrogel Scaffold Improved the Survival of Transplanted Stem Cells and Tissue Regeneration. [Abstract]

2018 Jan 1;8(4):878-893. PMID: 29463988

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Jan 1;8(4):878-893. [Abstract]

Accumulation of immune cells in host mice. Immunofluorescent images of CD4+ cells (green) in transplanted site in the normal, E+R, E+R+T, and E+R+T-RNPs groups at day 7 and day 21.
Biomaterials

Targeted regulation of lymphocytic ER stress response with an overall immunosuppression to alleviate allograft rejection. [Abstract]

2021 May:272:120757. PMID: 33798960
J Nanobiotechnology

RGD-HSA-TAC nanoparticles targeted delivery of tacrolimus and attenuation of podocyte injury in diabetic kidney disease. [Abstract]

2025 Feb 4;23(1):81. PMID: 39905421
J Control Release

Target-oriented delivery of self-assembled immunosuppressant cocktails prolongs allogeneic orthotopic liver transplant survival. [Abstract]

2020 Dec 10;328:237-250. PMID: 32866593
Pharmacol Res

Multiple microRNAs regulate tacrolimus metabolism through CYP3A5. [Abstract]

2021 Feb:164:105382. PMID: 33348024
Cell Mol Biol Lett

lncRNA Oip5-as1 inhibits excessive mitochondrial fission in myocardial ischemia/reperfusion injury by modulating DRP1 phosphorylation. [Abstract]

2024 May 14;29(1):72. PMID: 38745296
Mater Today Bio

3D in vitro synovial hyperplasia model on polycaprolactone-micropatterned nanofibrous microwells for screening disease-modifying anti-rheumatic drugs. [Abstract]

2024 Apr 22:26:101061. PMID: 38711937
Cancer Lett

FPR3 reprograms glycolytic metabolism and stemness in gastric cancer via calcium-NFATc1 pathway. [Abstract]

2024 Jul 1:593:216841. PMID: 38614385
Int J Biol Sci

Heterophyllin B enhances transcription factor EB-mediated autophagy and alleviates pyroptosis and oxidative stress after spinal cord injury. [Abstract]

2024 Oct 7;20(14):5415-5435. PMID: 39494322
J Colloid Interface Sci

Efficient local delivery of FK506 using blocking patches in psoriasis. [Abstract]

2023 Jan 15;630(Pt A):676-687. PMID: 36274404
Burns Trauma

Flufenamic acid inhibits pyroptosis in ischemic flaps via the AMPK-TRPML1-Calcineurin signaling pathway. [Abstract]

2025 Feb 17:13:tkaf007. PMID: 40655077
Acta Biomater

Oral delivery of ultra-small zwitterionic nanoparticles to overcome mucus and epithelial barriers for macrophage modulation and colitis therapy. [Abstract]

2025 Apr:196:399-409. PMID: 39983856
Proc Natl Acad Sci U S A

Calcineurin controls proximodistal blastema polarity in zebrafish fin regeneration. [Abstract]

2021 Jan 12;118(2):e2009539118. PMID: 33376206
Nano Lett

Route to Rheumatoid Arthritis by Macrophage-Derived Microvesicle-Coated Nanoparticles. [Abstract]

2019 Jan 9;19(1):124-134. PMID: 30521345
Nano Res

11, 6086-6101(2018).
Cell Commun Signal

Zinc-mediated activation of CREB pathway in proliferation of pulmonary artery smooth muscle cells in pulmonary hypertension. [Abstract]

2021 Oct 11;19(1):103. PMID: 34635097
Int J Biol Macromol

Nanoparticle-mediated calmodulin dsRNA and cyantraniliprole co-delivery system: High-efficient control of two key pear pests while ensuring safety for natural enemy insects. [Abstract]

2024 Aug 3:134478. PMID: 39102908
Acta Pharmacol Sin

Restoration of HMGCS2-mediated ketogenesis alleviates tacrolimus-induced hepatic lipid metabolism disorder. [Abstract]

2024 May 17. PMID: 38760545
Am J Transplant

miR-449a ameliorates acute rejection after liver transplantation via targeting procollagen-lysine1,2-oxoglutarate5-dioxygenase 1 in macrophages. [Abstract]

2023 Mar;23(3):336-352. PMID: 36695693
Drug Deliv

Immunosuppressive effect of PLGA-FK506-NPs in treatment of acute cardiac rejection via topical subcutaneous injection. [Abstract]

2021 Dec;28(1):1759-1768. PMID: 34463172
Mater Design

2023 Nov, 235, 112415.
Hepatobiliary Surg Nutr

Influence of immunosuppressive drugs on natural killer cells in therapeutic drug exposure in liver transplantation. [Abstract]

2023 Dec 1;12(6):835-853. PMID: 38115918
Br J Pharmacol

Regenerating islet-derived protein 3 gamma (Reg3g) ameliorates tacrolimus-induced pancreatic β-cell dysfunction in mice by restoring mitochondrial function. [Abstract]

2022 Jun;179(12):3078-3095. PMID: 35060126
Cell Syst

A Library of Phosphoproteomic and Chromatin Signatures for Characterizing Cellular Responses to Drug Perturbations. [Abstract]

2018 Apr 25;6(4):424-443.e7. PMID: 29655704
Aging Dis

ROR2-Related Skeletal Dysplasia Reveals Disrupted Chondrocyte Polarity through Modulation of BMP/TGF-β Signaling. [Abstract]

2024 Feb 1;15(1):282-294. PMID: 37307827
Cell Rep

TRESK channel contributes to depolarization-induced shunting inhibition and modulates epileptic seizures. [Abstract]

2021 Jul 20;36(3):109404. PMID: 34289346
NPJ Regen Med

Transplantation of PSC-derived myogenic progenitors counteracts disease phenotypes in FSHD mice. [Abstract]

2022 Sep 2;7(1):43. PMID: 36056021
Elife

2023 MAy 19.
Fundam Res

2024 Mar 19.
J Agric Food Chem

FK506 Targets MoFpr1 to Modulate Autophagy and Ubiquitination, Inhibiting the Pathogenicity of Magnaporthe oryzae. [Abstract]

2025 Jun 18;73(24):14985-15002. PMID: 40490869
Cell Biol Toxicol

Inhibition of calpain reduces cell apoptosis by suppressing mitochondrial fission in acute viral myocarditis. [Abstract]

2022 Jun;38(3):487-504. PMID: 34365571

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: Cell Biol Toxicol. 2022 Jun;38(3):487-504. [Abstract]

FK506 inhibits dephosphorylation of Drp-1 at Ser637 site induced by CVB3 infection. CVB3 infection-induced decrease in Bcl-2 expression and enhanced levels of Bax and Caspase-3 cleavage are reversed by FK506.
Biomater Sci

Electrospun polymer fibers modified with FK506 for the long-term treatment of acute cardiac allograft rejection in a heart transplantation model. [Abstract]

2023 May 30;11(11):4032-4042. PMID: 37129635
Biomater Sci

Bioinspired β-glucan microcapsules deliver FK506 to lymph nodes for treatment of cardiac allograft acute rejection. [Abstract]

2020 Oct 7;8(19):5282-5292. PMID: 32749395
Acta Physiol

Tacrolimus Induced Hypertension and Vascular Remodeling Includes Mechanisms of Cellular Senescence-The Protective Effect of Valsartan. [Abstract]

2026 Apr;242(4):e70189. PMID: 41814130
Cell Prolif

WNT16b promotes the proliferation and self-renewal of human limbal epithelial stem/progenitor cells via activating the calcium/calcineurin A/NFATC2 pathway. [Abstract]

2023 Oct;56(10):e13460. PMID: 36974338

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2023 Oct;56(10):e13460. [Abstract]

FK506 (5 μM; 14 days) significantly inhibits the protein expression of both calcineurin A and NFATC2 in hLESCs.

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2023 Oct;56(10):e13460. [Abstract]

FK506 (5 μM; 14 days) inhibits WNT16b on hLESC cell proliferation.

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2023 Oct;56(10):e13460. [Abstract]

FK506 (5 μM; 14 days) significantly inhibits the expression of WNT16b-promoting cell proliferation marker Ki67 and the putative hLESC marker ΔNp63α in hLESCs.
ACS Biomater Sci Eng

Mechanoresponsive Drug Loading System with Tunable Host-Guest Interactions for Ocular Disease Treatment. [Abstract]

2022 Nov 14;8(11):4850-4862. PMID: 36214483
J Ethnopharmacol

Elephantopus scaber suppresses ConA-induced T cell activation by inhibiting NF-κB and Ca2+/NFAT signaling. [Abstract]

2026 May 10:362:121364. PMID: 41687940
Food Funct

Sulforaphane protects microvascular endothelial cells in lower limb ischemia/reperfusion injury mice. [Abstract]

2023 Jul 31;14(15):7176-7194. PMID: 37462424
Int J Pharm

Tannic acid-modified FK506-loaded nanoparticles targeting lymph nodes for acute heart transplant rejection treatment. [Abstract]

2025 Jan 20:125247. PMID: 39842736
Int J Pharm

Delivery of FK506-loaded PLGA nanoparticles prolongs cardiac allograft survival. [Abstract]

2019 Dec 13;575:118951. PMID: 31843550
Int J Mol Sci

Enhanced Diaphragm Muscle Function upon Satellite Cell Transplantation in Dystrophic Mice. [Abstract]

2024 Feb 21;25(5):2503. PMID: 38473751
Int J Mol Sci

Expression of the Calcium-Binding Protein CALB1 Is Induced and Controls Intracellular Ca2+ Levels in Senescent Cells. [Abstract]

2022 Aug 19;23(16):9376. PMID: 36012633
Biomolecules

Human Menstrual Blood-Derived Stem Cells Protect against Tacrolimus-Induced Islet Dysfunction via Cystathionine β-Synthase Mediated IL-6/STAT3 Inactivation. [Abstract]

2024 Jun 8;14(6):671. PMID: 38927074
Int Immunopharmacol

Gambogenic acid suppresses T cell proliferation via inhibition of ERK signaling pathway. [Abstract]

2026 May 15:177:116529. PMID: 41871492
Int Immunopharmacol

Repurposing zafirlukast confers renal protection in ischemia-reperfusion injury via suppressing macrophage METosis. [Abstract]

2025 Sep 8:165:115459. PMID: 40925201
Invest Ophthalmol Vis Sci

Effect of TRPM8 Functional Loss on Corneal Epithelial Wound Healing in Mice. [Abstract]

2023 Jan 3;64(1):19. PMID: 36692471
Hepatobiliary Pancreat Dis Int

HSP110 aggravates ischemia-reperfusion injury after liver transplantation by promoting NF-κB pathway. [Abstract]

2024 Aug;23(4):344-352. PMID: 37648554
Skelet Muscle

Efficient engraftment of pluripotent stem cell-derived myogenic progenitors in a novel immunodeficient mouse model of limb girdle muscular dystrophy 2I. [Abstract]

2020 Apr 22;10(1):10. PMID: 32321586
Biochim Biophys Acta Mol Basis Dis

IL-10 alleviates aTCMR by inhibiting NFATc1 signaling pathway of T cells after kidney transplantation. [Abstract]

2025 Apr 21;1871(6):167857. PMID: 40268206
FASEB J

3,4-Dimethoxychalcone alleviates limb ischemia/reperfusion injury by TFEB-mediated autophagy enhancement and antioxidative response. [Abstract]

2025 Apr 15;39(7):e70496. PMID: 40162605
FASEB J

Glycyrrhizic acid improves tacrolimus-induced renal injury by regulating autophagy. [Abstract]

2023 Feb;37(2):e22749. PMID: 36688808
Mediators Inflamm

Concomitant Treatment with Etanercept and Tacrolimus Synergistically Attenuates Arthritis Progression via Inhibition of Matrix Metalloproteinase-3 Production and Osteoclastogenesis in Human TNF- α Transgenic Mice. [Abstract]

2019 Dec 17;2019:4176974. PMID: 31949424
Toxics

Evaluation of THP-1 and Jurkat Cell Lines Coculture for the In Vitro Assessment of the Effects of Immunosuppressive Substances. [Abstract]

2024 Aug 19;12(8):607. PMID: 39195709

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: Toxics. 2024 Aug 19;12(8):607. [Abstract]

Tacrolimus monohydrate (100 nM-10 µM) decreased IL-2 secretion from Jurkat cells and coculture with THP-1 cells.

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: Toxics. 2024 Aug 19;12(8):607. [Abstract]

Tacrolimus monohydrate (100 nM-10 µM) caused significant TNFα inhibition in Jurkat cells and coculture with THP-1 cells.

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: Toxics. 2024 Aug 19;12(8):607. [Abstract]

Tacrolimus monohydrate (100 nM-10 µM) significantly inhibited IL-8 secretion from THP-1, Jurkat cells and their coculture.
Antiviral Res

Codelivery of Cas9 mRNA and guide RNAs edits hepatitis B virus episomal and integration DNA in mouse and tree shrew models. [Abstract]

2023 Jul:215:105618. PMID: 37142191
J Neurochem

Continued P2X7 activation leads to mitochondrial fission and compromising microglial phagocytosis after subarachnoid haemorrhage. [Abstract]

2022 Dec;163(5):419-437. PMID: 36269673
Toxins

Effects of Destruxin A on Silkworm's Immunophilins. [Abstract]

2019 Jun 18;11(6):349. PMID: 31216655
Cell Signal

Inhibition of ferroptosis rescues BMP osteogenic differentiation impaired by iron overload in the osteoporotic microenvironment. [Abstract]

2025 Sep 8:136:112116. PMID: 40930476
J Cell Sci

FKBP12 mediates necroptosis by initiating RIPK1-RIPK3-MLKL signal transduction in response to TNF receptor 1 ligation. [Abstract]

2019 May 20;132(10):jcs227777. PMID: 31028177
Mol Med Rep

P2X7 receptor knockdown suppresses osteoclast differentiation by inhibiting autophagy and Ca2+/calcineurin signaling. [Abstract]

2022 May;25(5):160. PMID: 35266012
J Immunol

IL-2 complex therapy prolongs fully MHC-mismatched murine cardiac allograft survival. [Abstract]

2025 Dec 10:vkaf303. PMID: 41369981
Vaccines

Comparative Ability of Various Immunosuppressants as Adjuvants on the Activity of T1D Vaccine. [Abstract]

2024 Sep 29;12(10):1117. PMID: 39460283
Wound Repair Regen

Drug suspending during wound healing effectively weakens immunosuppression-related complications by preserving CD8+ T cell function. [Abstract]

2023 Jul-Aug;31(4):489-499. PMID: 37129099
Animal Model Exp Med

Anti-inflammatory effects of amarogentin on 2,4-dinitrochlorobenzene-induced atopic dermatitis-like mice and in HaCat cells. [Abstract]

2023 Jun;6(3):255-265. PMID: 36131559
Dis Model Mech

Yeast-model-based study identified myosin- and calcium-dependent calmodulin signalling as a potential target for drug intervention in chorea-acanthocytosis. [Abstract]

2019 Jan 28;12(1). pii: dmm036830. PMID: 30635263
Pathol Res Pract

Combined treatment of tacrolimus and pirfenidone effectively improves BLM-induced pulmonary fibrosis in mice by inhibiting the TGFβ1/Smad2/3 signaling. [Abstract]

2025 Aug:272:156095. PMID: 40617191
J Pharm Biomed Anal

Determination of five mTOR inhibitors in human plasma for hepatocellular carcinoma treatment using QuEChERS-UHPLC-MS/MS. [Abstract]

2023 Oct 25:235:115652. PMID: 37633163
Insect Sci

Cytoplasmic FKBPs are involved in molting and metamorphosis through regulating the nuclear localization of EcR. [Abstract]

2024 Jun;31(3):759-772. PMID: 37822278
Clin Transl Sci

Inhibition of Tacrolimus Metabolism by Cannabidiol and Its Metabolites In Vitro. [Abstract]

2025 Feb;18(2):e70152. PMID: 39921332
BMC Immunol

Tacrolimus reverses pemphigus vulgaris serum-induced depletion of desmoglein in HaCaT cells via inhibition of heat shock protein 27 phosphorylation. [Abstract]

2023 Nov 8;24(1):43. PMID: 37940861
BMC Pharmacol Toxicol

The effect of tacrolimus-induced toxicity on metabolic profiling in target tissues of mice. [Abstract]

2022 Nov 28;23(1):87. PMID: 36443830
Ultrasound Med Biol

Amplification of Plasma MicroRNAs for Non-invasive Early Detection of Acute Rejection after Heart Transplantation With Ultrasound-Targeted Microbubble Destruction. [Abstract]

2023 Jul;49(7):1647-1657. PMID: 37120328
Brain Res

Dephosphorylation by calcineurin regulates translocation of dynamin-related protein 1 to mitochondria in hepatic ischemia reperfusion induced hippocampus injury in young mice. [Abstract]

2019 May 15:1711:68-76. PMID: 30659828

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: Brain Res. 2019 May 15:1711:68-76. [Abstract]

Levels of CytC in cytosol (Cyto-CytC), CytC in mitochondria (Mito- CytC) and cleaved caspase-3 in hippocampus are determined by western blot with the treatment of sham, HIR, MDV or FK506.
Acta Trop

Tacrolimus, a rapamycin target protein inhibitor, exerts anti-cystic echinococcosis effects both in vitro and in vivo. [Abstract]

2020 Dec;212:105708. PMID: 32956634
J Viral Hepat

The Differential Effects of Immunosuppressants on Hepatitis E Virus Replication and the Triggered Inflammatory Responses in Macrophages. [Abstract]

2026 Jan;33(1):e70118. PMID: 41400072
Biochim Biophys Acta Gen Subj

miR-731 modulates the zebrafish heart morphogenesis via targeting Calcineurin/Nfatc3a pathway. [Abstract]

2022 Jun;1866(6):130133. PMID: 35346765
J Toxicol Sci

Validation of a new protocol for a zebrafish MEFL (malformation or embryo-fetal lethality) test method that conforms to the ICH S5 (R3) guideline. [Abstract]

2024;49(8):337-348. PMID: 39098043
Transpl Immunol

Diphenyleneiodonium ameliorates acute liver rejection during transplantation by inhibiting neutrophil extracellular traps formation in vivo. [Abstract]

2021 Oct:68:101434. PMID: 34216758
J Vet Med Sci

Detection of anti-feline infectious peritonitis virus activity of a Chinese herb extract using geneLEAD VIII, a fully automated nucleic acid extraction/quantitative PCR testing system. [Abstract]

2023 Mar 30;85(4):443-446. PMID: 36806247
Northwestern University

2026.
SSRN

2026 May 28.
Res Sq

2026 Mar 27.
Res Sq

2025 Dec 17.
Seoul National University

2033.
bioRxiv

2025 Nov 20.
Preprints

2025 Sep 24.
Developments and Experiments in Health and Medicine

2025.
Indiana University

2025.
bioRxiv

Cannabidiol exerts anti-inflammatory effects but maintains T effector memory cell differentiation: A Single-Cell Study in Humans. [Abstract]

2025 Jul 31:2025.07.30.667742. PMID: 40766582
bioRxiv

2025 February 01.
Res Sq

Pharmacokinetics and Pharmacogenomics of Ribociclib in Black Patients with Metastatic Breast Cancer: The LEANORA study. [Abstract]

2024 Aug 13:rs.3.rs-4656461. PMID: 39184092
SSRN

2023 Oct 31.

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: SSRN. 2023 Oct 31.

Tacrolimus monohydrate (FK506) (100 ng/mL) significantly increased the expressions of protein K14, CDH1 in kCSTA cells in an inflammatory environment.

Tacrolimus monohydrate purchased from MedChemExpress. Usage Cited in: SSRN. 2023 Oct 31.

Tacrolimus monohydrate (FK506) (100 ng/mL) increased CSTA proteins in kCSTA cells.
Hong Kong Polytechnic University

2023 Apr.
Patent

US20220087984A1.
Research Square Preprint

2020 Dec.
Patent

US20180263995A1.
Am J Dig Dis (Madison)

2015;2(2):95-99.
Int J Physiol Pathophysiol Pharmacol

The mTOR inhibitor sirolimus suppresses renal, hepatic, and cardiac tissue cellular respiration. [Abstract]

2015 Mar 20;7(1):54-60. PMID: 26069529

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (121.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.2165 mL

6.0825 mL

12.1650 mL

5 mM

0.2433 mL

1.2165 mL

2.4330 mL

10 mM

0.1217 mL

0.6083 mL

1.2165 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[3]

Tumor cell proliferation is determined by the MTT assay. Briefly, after MH3924A cells have reached the logarithmic growth phase, a 0.2-mL cell suspension at 1×10⁴ cells/mL is added into each well of a 96-well plate and cultured in DMEM with 10% FBS, 10 μg/L vascular endothelial growth factor and 0.1 g/L heparin for 24 h. When adherent growth is established, different concentrations of Tacrolimus (10, 100 and 1,000 μg/L) , AMD3100 (10, 50 and 100 μg/L) and Tacrolimus (0 and 100 μg/L)+AMD3100 (0, 10, 50 and 100 μg/L) are added into the plates. Untreated cells cultured in medium alone are used as controls. After culturing for 48 h, 10 μL MTT (5 g/L) are added, and each well is incubated for 6 h; next, 150 μL/well DMSO are added, followed by measurements of the absorbance at 570 mm on a spectrophotometer reader. Each well is measured three times, and each sample is assayed in triplicate^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[4]

Mice^[4]
Six-week-old male C57BL/6J mice are maintained in a temperature- and humidity-controlled room with a 12-h light-dark cycle. For the multiple dosing study, colitic mice (n=10) are orally administered Tacrolimus at 30 mg/kg for 7 d (Days 10 to 16) or 14 d (Days 10 to 23). Control (n=10) and normal groups (n=5) are administered placebo using the same regimen. Tacrolimus or placebo is administered at 10 mL/kg. Mice are euthanized by CO₂ inhalation on the day following the final dosing. For the single dosing study, colitic mice are orally administered Tacrolimus at 30 mg/kg or placebo (n=8) once on Day 7, 10, 17, or 24. Normal mice (n=4) are administered placebo using the same regimen. Mice are euthanized by CO₂ inhalation eight hours after dosing^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (480 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

[2]. 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. [Content Brief]

[3]. 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. [Content Brief]

[4]. 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. [Content Brief]

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

[6]. Soini L, et al. Molecular glues to stabilise protein-protein interactions. Curr Opin Chem Biol. 2022 Aug;69:102169. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.2165 mL	6.0825 mL	12.1650 mL	30.4125 mL
	5 mM	0.2433 mL	1.2165 mL	2.4330 mL	6.0825 mL
	10 mM	0.1217 mL	0.6083 mL	1.2165 mL	3.0413 mL
	15 mM	0.0811 mL	0.4055 mL	0.8110 mL	2.0275 mL
	20 mM	0.0608 mL	0.3041 mL	0.6083 mL	1.5206 mL
	25 mM	0.0487 mL	0.2433 mL	0.4866 mL	1.2165 mL
	30 mM	0.0406 mL	0.2028 mL	0.4055 mL	1.0138 mL
	40 mM	0.0304 mL	0.1521 mL	0.3041 mL	0.7603 mL
	50 mM	0.0243 mL	0.1217 mL	0.2433 mL	0.6083 mL
	60 mM	0.0203 mL	0.1014 mL	0.2028 mL	0.5069 mL
	80 mM	0.0152 mL	0.0760 mL	0.1521 mL	0.3802 mL
	100 mM	0.0122 mL	0.0608 mL	0.1217 mL	0.3041 mL

Keywords

Tacrolimus monohydrate

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Tacrolimus monohydrate

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