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Mizoribine

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Chemical Structure| 50924-49-7 同义名 : 咪唑立宾 ;NSC 289637;HE 69;Bredinin
CAS号 : 50924-49-7
货号 : A306960
分子式 : C9H13N3O6
纯度 : 98%
分子量 : 259.216
MDL号 : MFCD00057221
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(231.47 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
动物实验配方：
生物活性
描述 Mizoribine (Bredinin, MZB) is an immunosuppressive drug used in renal transplantation, IgA nephropathy, lupus erythematosus and childhood nephrotic syndrome[1]. After entering into cells, Mizoribine can firstly be phosphorylated to become its active form, Mizoribine 5’-monophosphate (MZ-5-P) by adenosine kinase. Then, MZ-5-P, the active form of Mizoribine, can selectively inhibit inosine monophosphate (IMP) dehydrogenase (ki = 10 nM) and guanosine monophosphate (GMP) synthetase (ki = 10 μM) [1], which are required for synthesis of GMP from IMP in de novo way. The immunosuppressive effect of Mizoribine on T cells may due to specific perturbation of guanine nucleotide, the second messengers in T cell activation, caused by Mizoribine. Meanwhile, Mizoribine can also prevent cells from exiting G1 phase and entering S phase by blocking T cell proliferation via a guanine nucleotide-dependent mechanism, which further contributes to its effect on immunosuppression[2].
作用机制 Mizoribine can inhibit T cell activation both through perturbation of guanine nucleotide and anti-proliferation[2].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02256150 Lupus Nephritis Phase 3 Active, not recruiting March 2019 -
NCT02257697 Nephrotic Syndrome Phase 3 Active, not recruiting November 2018 -
NCT02373202 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.86mL

0.77mL

0.39mL

19.29mL

3.86mL

1.93mL

38.58mL

7.72mL

3.86mL
参考文献

[1]Kawasaki Y, et al. Mizoribine: a new approach in the treatment of renal disease. Clin Dev Immunol. 2009;2009:681482.

[2]Dayton JS, Turka LA, et al. Comparison of the effects of mizoribine with those of azathioprine, 6-mercaptopurine, and mycophenolic acid on T lymphocyte proliferation and purine ribonucleotide metabolism. Mol Pharmacol. 1992 Apr;41(4):671-6.

[3]Kamada H, Nakagami K, et al. Effect of mizoribine on collagen-induced arthritis in mice. Jpn J Pharmacol. 1996 Feb;70(2):169-75.

[4]Valvezan AJ, Turner M, et al. mTORC1 Couples Nucleotide Synthesis to Nucleotide Demand Resulting in a Targetable Metabolic Vulnerability. Cancer Cell. 2017 Nov 13;32(5):624-638.e5.

[5]Chen DY, Kikuchi H, et al. Evaluation of mizoribine as an immunosuppressant in subrenal capsule assay using immunocompetent mice. Jpn J Cancer Res. 1990 Feb;81(2):183-7.

[6]Murakami T, Mori N, et al. Involvement of Multiple Transporters-mediated Transports in Mizoribine and Methotrexate Pharmacokinetics. Pharmaceuticals (Basel). 2012 Aug 10;5(8):802-36.