Mycophenolate Mofetil

Catalog No.S1501 Synonyms: RS61443

Mycophenolate Mofetil Chemical Structure

Molecular Weight(MW): 433.49

Mycophenolate Mofetil is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively.

Size Price Stock Quantity  
In DMSO USD 130 In stock
USD 97 In stock
USD 170 In stock
USD 270 In stock
USD 970 In stock
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4 Customer Reviews

  • Young 9 week of age pre-diseased (Pre) mice kidneys were collected and served as a healthy control group. Representative pictures of the histological results are shown (E).

    Clin Immunol, 2016, 164:65-77. Mycophenolate Mofetil purchased from Selleck.

    Natural killer cell activation is differentially modulated by treatment with CsA,Tac, Sir, or MMF. PBMC of three or four healthy donors were incubated for 4 days with or without 500 U/ml IL-2 in the presence CNI (CsA and Tac), mTORi (Sir), or mycophenolate (MMF) at a concentration of 10 µM, DMSO control solvent or medium.The percentage of all NK cells (CD3− /CD56+ ) and of the major NK cell subsets defined as CD16+ /CD16− CD56dim and CD56bright were determined by flow cytometry. Each data point indicates one donor, and the median values with standard deviations are depicted as black bars.

    Front Immunol 2013 4, 46. Mycophenolate Mofetil purchased from Selleck.

  • Natural killer cell activation is differentially modulated by treatment with CsA,Tac, Sir, or MMF. PBMC of three or four healthy donors were incubated for 4 days with or without 500 U/ml IL-2 in the presence CNI (CsA and Tac), mTORi (Sir), or mycophenolate (MMF) at a concentration of 10 µM, DMSO control solvent or medium.The percentage of as well as CD69+ NK cells were determined by flow cytometry. Each data point indicates one donor, and the median values with standard deviations are depicted as black bars.

    Front Immunol 2013 4, 46. Mycophenolate Mofetil purchased from Selleck.

    Natural killer cell activation is differentially modulated by treatment with CsA,Tac, Sir, or MMF. PBMC of three or four healthy donors were incubated for 4 days with or without 500 U/ml IL-2 in the presence CNI (CsA and Tac), mTORi (Sir), or mycophenolate (MMF) at a concentration of 10 µM, DMSO control solvent or medium.The percentage of CD25+ NK cells were determined by flow cytometry. Each data point indicates one donor, and the median values with standard deviations are depicted as black bars.

    Front Immunol 2013 4:, 46. Mycophenolate Mofetil purchased from Selleck.

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Biological Activity

Description Mycophenolate Mofetil is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively.
Targets
Inosine monophosphate dehydrogenase II [1]
(Cell-free assay)
Inosine monophosphate dehydrogenase I [1]
(Cell-free assay)
27 nM 39 nM
In vitro

Mycophenolate mofetil is an ester prodrug of the active immunosuppressant mycophenolic acid (MPA). The latter shows a noncompetitive, selective and reversible inhibition activity against inosine monophosphate dehydrogenase type I/II with IC50 of 39 nM and 27 nM, respectively. Moreover, MPA also produces the concentration-dependent inhibition of proliferation of ConA-stimulated T cells, LPS-stimulated B cells and alloantigen-specific T cells with IC50 of 100 nM, 120 nM, and 51 nM, respectively. [1] Mycophenolate mofetil with high concentration of 10 μg/mL induces a strong apoptosis in microglial cell cultures and increases the number of activated caspase-3 immunoreactive apoptotic cells. In addition, Mycophenolate mofetil (1 μg/mL) strongly inhibits proliferation of both microglial cells and astrocytes. [2] A recent study shows that Mycophenolate mofetil significantly attenuates the extent of neuronal cell death of organotypic hippocampal slice cultures after neuronal injury in a time-dependent manner. [4]

In vivo In an ACI-to-Lewis rat heterotopic cardiac transplant model, treatment of Mycophenolate mofetil at doses of 20 mg/kg and 40 mg/kg leads to a prolongation of graft survival, with median survival time (MST) of 14.5 days and 18.5 days, respectively. [1] In bleomycin (BLM)-induced scleroderma mouse model, Mycophenolate mofetil reduces inflammatory-cell infiltration, tissue hydroxyproline content and dermal thickness. [3]

Protocol

Kinase Assay:[1]
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IMP dehydrogenase Types I and II enzymatic activity:

IMP dehydrogenase Types I and II are purified from E. coli expressing human enzymes. The assay is performed using a flat bottom, UV-transparent 96-well plate. The final 200 μL reaction mixture contained 0.1 M Tris, 0.1 M KCl, 3 mM EDTA pH 8.0, 2 mM DTT, and 40 nM of either IMP dehydrogenase Type I or Type II. The reaction is initiated by adding 400 μM NAD and 400 μM IMP, followed by incubation at 37 °C for 2.5 hours. The reaction rate of the conversion of NAD to NADH is then measured based on the increase in absorbance at 340 nm. The assays are also performed in the presence of 50% human serum to estimate serum protein binding by different IMP dehydrogenase inhibitors.
Cell Research:[1]
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  • Cell lines: ConA-stimulated T cells and LPS-stimulated B cells
  • Concentrations: 0 to 10 μM
  • Incubation Time: 48 hours
  • Method: The spleens of male Lewis rats aged 8 weeks are aseptically removed and teased into single-cell suspensions, and the resulting splenocytes are suspended in RPMI1640 medium containing 10% fetal calf serum, 100 U/mL penicillin, and 100 μg/mL streptomycin. Assays are performed in flat-bottomed microtiter plates, with each well containing 150000 splenocytes in a total volume of 100 μL. Splenocytes are incubated in medium containing either 1 μg/mL Concanavalin A (ConA) or lipopolysaccharide (LPS) as T or B cell mitogen, respectively, along with various concentrations of MPA at 37 °C for 48 hours in a humidified atmosphere of 5% CO2-95% air. During the final 6 hours of incubation, cells are pulsed with 1 μCi of 3H-thymidine/well, and harvested onto pressed fiberglass in a cell harvester. The uptake of 3H-thymidine by proliferating cells is measured using a liquid scintillation counter. The in vitro immune response of alloantigen-specific T cells is evaluated as a proliferation response using one-way mixed lymphocyte reaction assay. Mesenteric lymph nodes cells from male Lewis rats aged 8 weeks and splenocytes from male ACI rats aged 8 weeks are used as responder and stimulator cells, respectively. Single-cell suspensions are prepared, and the responder cells are cultured with irradiated (20 Gy) stimulator cells in RPMI1640 supplemented with 10% fetal calf serum, 100 U/mL penicillin and 100 μg/mL streptomycin, in 96-well plates (U-bottom) and in the presence of various concentrations of MPA (total volume: 200 μL, 37 °C, 5% CO2 humidified atmosphere, 72 hours). As a negative control, responder cells are cultured with irradiated splenocytes of Lewis rats. The cell proliferation is quantified by the uptake of 3H-thymidine.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Lewis rats with abdominal vascularized heterotopic cardiac transplantation.
  • Formulation: Mycophenolate mofetil is dissolved in 0.5% methylcellulose water.
  • Dosages: ≤40 mg/kg
  • Administration: Administered via i.v.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (198.38 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
0.5% methylcellulose
20 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 433.49
Formula

C23H31NO7

CAS No. 128794-94-5
Storage powder
Synonyms RS61443

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01503242 Recruiting Plasma Cell Myeloma|Refractory Plasma Cell Myeloma Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) January 9, 2012 Phase 1
NCT02782546 Recruiting Acute Myeloid Leukemia Washington University School of Medicine January 30, 2017 Phase 2
NCT02423915 Recruiting Leukemia|Lymphoma M.D. Anderson Cancer Center|National Cancer Institute (NCI)|Targazyme, Inc.|Cancer Prevention Research Institute of Texas July 30, 2015 Phase 1|Phase 2
NCT00425802 Completed Leukemia|Lymphoma Memorial Sloan Kettering Cancer Center|National Cancer Institute (NCI) November 28, 2006 Phase 2
NCT01701986 Recruiting Lymphoma M.D. Anderson Cancer Center October 25, 2012 Phase 1|Phase 2
NCT00723099 Suspended Acute Biphenotypic Leukemia|Acute Lymphoblastic Leukemia|Acute Myeloid Leukemia|Aggressive Non-Hodgkin Lymphoma|Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Indolent Non-Hodgkin Lymphoma|Malignant Lymphoma, Large Cell Type|Mixed Phenotype Acute Leukemia|Myelodysplastic Syndrome|Myeloproliferative Neoplasm|Recurrent Chronic Lymphocytic Leukemia|Recurrent Follicular Lymphoma|Recurrent Lymphoplasmacytic Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Plasma Cell Myeloma|Recurrent Small Lymphocytic Lymphoma|Recurrent T-Cell Non-Hodgkin Lymphoma|Refractory Chronic Lymphocytic Leukemia|Refractory Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Refractory Follicular Lymphoma|Refractory Hodgkin Lymphoma|Refractory Lymphoplasmacytic Lymphoma|Refractory Mantle Cell Lymphoma|Refractory Small Lymphocytic Lymphoma|T-Cell Non-Hodgkin Lymphoma Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) June 25, 2008 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID