Mycophenolate mofetil (RS-61443)

Catalog No.S1501 Synonyms: Mycophenolic acid morpholinoethyl ester, CellCept, TM-MMF

For research use only.

Mycophenolate Mofetil (RS 61443, Mycophenolic acid morpholinoethyl ester, CellCept, TM-MMF) is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively. Mycophenolate Mofetil induces caspase-dependent apoptosis and cell cycle inhibition in multiple myeloma cells.

Mycophenolate mofetil (RS-61443) Chemical Structure

CAS No. 128794-94-5

Selleck's Mycophenolate mofetil (RS-61443) has been cited by 7 Publications

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Biological Activity

Description Mycophenolate Mofetil (RS 61443, Mycophenolic acid morpholinoethyl ester, CellCept, TM-MMF) is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively. Mycophenolate Mofetil induces caspase-dependent apoptosis and cell cycle inhibition in multiple myeloma cells.
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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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.

Animal Research:

[1]

  • Animal Models: Lewis rats with abdominal vascularized heterotopic cardiac transplantation.
  • Dosages: ≤40 mg/kg
  • Administration: oral administration

Solubility (25°C)

In vitro

DMSO 86 mg/mL
(198.38 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
0.5% methylcellulose
For best results, use promptly after mixing.

20 mg/mL

Chemical Information

Molecular Weight 433.49
Formula

C23H31NO7

CAS No. 128794-94-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C2COC(=O)C2=C(C(=C1OC)CC=C(C)CCC(=O)OCCN3CCOCC3)O

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05120570 Not yet recruiting Drug: VIC- 1911 Acute Leukemia|Myelodysplastic Syndromes|Myeloproliferative Neoplasm|Lymphoma Masonic Cancer Center University of Minnesota February 2022 Phase 1|Phase 2
NCT04630782 Recruiting Diagnostic Test: PET-MRI scan Systemic Sclerosis|Scleroderma Singapore General Hospital|National University Hospital Singapore|Tan Tock Seng Hospital|Changi General Hospital|Sengkang General Hospital|National University Singapore|Nanyang Technological University|Duke-NUS Graduate Medical School April 9 2020 --
NCT04360031 Recruiting Drug: Tacrolimus Kidney Transplant; Complications|Immunosuppression|Transplant Failure Université Catholique de Louvain February 10 2020 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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