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Mycophenolate Mofetil

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Chemical Structure| 128794-94-5 同义名 : 霉酚酸吗啉乙酯 ;RS 61443;TM-MMF;MMF;CellCept;Mycophenolic acid morpholinoethyl ester
CAS号 : 128794-94-5
货号 : A143691
分子式 : C23H31NO7
纯度 : 98%
分子量 : 433.495
MDL号 : MFCD00867568
存储条件:

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(242.22 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

1M NaOH: 30 mg/mL(69.2 mM),配合低频超声,并调节pH至12

动物实验配方:

0.5% methylcellulose+water 20 mg/mL suspension

生物活性
靶点
  • Dehydrogenase

    Inosine monophosphate dehydrogenase I, IC50:39 nM

    Inosine monophosphate dehydrogenase II, IC50:27 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.31mL

0.46mL

0.23mL

11.53mL

2.31mL

1.15mL

23.07mL

4.61mL

2.31mL

参考文献

[1]Dehghani F, Sayan M, et al. Inhibition of microglial and astrocytic inflammatory responses by the immunosuppressant mycophenolate mofetil. Neuropathol Appl Neurobiol. 2010 Dec;36(7):598-611.

[2]Nakanishi T, Morokata T, et al. Effect of the inosine 5'-monophosphate dehydrogenase inhibitor BMS-566419 on rat cardiac allograft rejection. Int Immunopharmacol. 2010 Jan;10(1):91-7.

[3]Zwerner J, Fiorentino D. Mycophenolate mofetil. Dermatol Ther. 2007 Jul-Aug;20(4):229-38

[4]Sievers TM, Rossi SJ, Ghobrial RM, Arriola E, Nishimura P, Kawano M, Holt CD. Mycophenolate mofetil. Pharmacotherapy. 1997 Nov-Dec;17(6):1178-97

[5]Sollinger HW. Mycophenolate mofetil. Kidney Int Suppl. 1995 Dec;52:S14-7