Inosine monophosphate dehydrogenase II, IC50:27 nM
Inosine monophosphate dehydrogenase I, IC50:39 nM
描述
Mycophenolate mofetil (MMF) is a relatively new systemic immunosuppressive agent used in the field of dermatologic[3]. It is the morpholinoethylester prodrug of mycophenolic acid, an agent that inhibits the proliferation of B and T lymphocytes through noncompetitive, reversible inhibition of inosine monophosphate dehydrogenase, a key enzyme in the de novo synthetic pathway of guanine nucleotides. Mycophenolate mofetil is approved for the prevention of acute renal allograft rejection when given in combination with cyclosporine and steroids[4]. A phase I clinical trial showed MMF was well tolerated in renal transplant patients at doses up to 3,500 mg/day for up to two years. There was no correlation between the incidence of adverse effects and dose of MMF, and no overt nephrotoxicity, hepatotoxicity, or myelotoxicity was observed. In a large multicenter trial, MMF in combination with cyclosporine and prednisone was superior to a standard immunosuppressive regimen including azathioprine[5].
Mycophenolate Mofetil/吗替麦考酚酯 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
MRL-(Fas)lpr mice
Spontaneous autoimmune tissue injury model
Oral
100 mg/kg
Daily administration for 8 weeks
To compare the therapeutic effects of Cat-S inhibitor RO5459072 and MMF on systemic autoimmunity and lupus nephritis. RO5459072 dose-dependently reversed aberrant systemic autoimmunity (e.g., plasma cytokines, activation of myeloid cells, and hypergammaglobulinemia) and significantly suppressed IgG autoantibody production. RO5459072 also dose-dependently improved the pathological scores and proteinuria in lupus nephritis, with effects superior to MMF.
Sci Rep. 2017 Jun 5;7(1):2775
C3H/HeNHsd mice
CBV3-induced myocarditis model
Oral gavage
100, 200 or 300 mg/kg/day
Twice daily for 7 consecutive days
Evaluate the protective effect of MMF on CBV3-induced myocarditis, results showed MMF significantly reduced the number of myocarditis foci
BMC Microbiol. 2003 Dec 21;3:25.
NZB/W F1 mice
Lupus nephritis model
Oral gavage
100 mg/kg
Once daily for 4 weeks
MMF significantly reduced serum CD44 and VCAM-1 levels to pre-nephritic levels, improving kidney inflammation and fibrosis
Front Immunol. 2024 Oct 1;15:1443153
MRL/lpr mice
Lupus nephritis model
Oral
50 mg/kg
Once daily for 8 weeks
To evaluate the efficacy of multitarget therapy (MT) in the treatment of lupus nephritis, results showed that MT therapy significantly improved systemic immune activation and renal injury.
EBioMedicine. 2025 Feb;112:105553
NZB/W F1 mice
Lupus nephritis model
Oral gavage
100 mg/kg
Daily administration for 24 weeks
To evaluate the therapeutic effect of mycophenolate mofetil on lupus nephritis. Results showed that mycophenolate mofetil significantly reduced proteinuria, improved survival, and attenuated tubulointerstitial inflammation and glomerular damage.
Arthritis Rheumatol. 2016 Nov;68(11):2740-2751
C3H mice
Immunosuppressed mouse model
Oral gavage
40 mg/kg
Daily for 13 days
To study the role of mycophenolate mofetil in an immunosuppressive regimen mimicking the state of lung transplant recipients.
Microbiol Spectr. 2025 Jan 7;13(1):e0176324
Mice
Myocardial infarction model
Intraperitoneal injection
20 mg/kg/day
Daily until analysis
Attenuate immune response and promote cardiac reprogramming
搜索
