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/ Mizoribine

咪唑利宾 /Mizoribine {[allProObj[0].p_purity_real_show]}

货号：A306960 同义名： 咪唑立宾 / NSC 289637;HE 69

Mizoribine是一种免疫抑制剂（IC50 = 100 μM），通过抑制 IMPDH 选择性地抑制淋巴细胞的增殖。

Mizoribine 化学结构 CAS号：50924-49-7
Mizoribine 化学结构
CAS号：50924-49-7
Mizoribine 3D分子结构
CAS号：50924-49-7
Mizoribine 化学结构 CAS号：50924-49-7
Mizoribine 3D分子结构 CAS号：50924-49-7
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Mizoribine 纯度/质量文件 产品仅供科研

货号：A306960 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 DNA synthesis ↓ helicase ↓ RdRp ↓ ribonucleotide reductase ↓ tRNA synthetase ↓ YB-1 ↓ 其他靶点 纯度
Fexinidazole ✔ 98%
Daptomycin ✔ 98%
Blasticidin S·HCl ✔ 98%
Metronidazole ✔ 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

 		98%
Triglycidyl isocyanurate ✔ p53 98+%
Nedaplatin ✔ 99%+
Bendamustine ✔ 98+%
Trifluridine ✔ 98%
Robinetin ✔ 99%+
Carboplatin ✔ 99%
Cidofovir ✔ 99%
Cisplatin ✔ 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

 		98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

 		99%+
Oxaliplatin ✔ 98%
YK-4-279 ✔ 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

 		99%+
RK-33 ✔ 98%
Brr2-IN-3 ✔ 99%+
Phen-DC3 Trifluoromethanesulfonate ✔ 98%
Favipiravir ✔ 99%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

 		99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

 		97%
Didox ✔ 98%
(E)-3-AP ✔ 99%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

 		99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, Kd: 42.1 nM

Leucyl-tRNA synthetase, IC50: 46.11 nM

 		98%
SU056 +

YB-1, IC50: 1.73 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Mizoribine 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].

Mizoribine 动物研究

Dose Mice: 10 mg/kg[3] (i.d.), max = 200 mg/kg[4] (i.p.), max = 400 mg/kg[5] (s.c.)
Administration i.d., i.p., s.c.
Pharmacokinetics
Animal Rats[6]
Dose 9 mg/kg
Administration p.o.
Tmax 1.5 h

Mizoribine 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 - -

Mizoribine 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.

Mizoribine 实验方案

计算器
存储液制备 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

Mizoribine 技术信息

CAS号50924-49-7
分子式C9H13N3O6
分子量 259.216
别名 咪唑立宾 ;NSC 289637;HE 69;Bredinin
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C
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

Tags: Mizoribine | NSC 289637;HE 69;Bredinin | 咪唑立宾 | Antivirus | DNA/RNA Synthesis | AmBeed-信号通路专用抑制剂 | Mizoribine 纯度/质量文件 | Mizoribine 亚型比较 | Mizoribine 生物活性 | Mizoribine 动物研究 | Mizoribine 临床数据 | Mizoribine 参考文献 | Mizoribine 实验方案 | Mizoribine 技术信息

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