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CAS No.: 50924-49-7

咪唑利宾 Catalog No. CSN11454

Synonyms: NSC 289637;HE 69;β-Bredinin

Mizoribine is an immunosuppressive agents (IC50=100 μM) that inhibit the proliferation of lymphocytes selectively, via inhibition of IMPDH.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 IMPDH

IC50:100μM
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].
动物研究
剂量
Mice: 10 mg/kg^[3] (i.d.), max = 200 mg/kg^[4] (i.p.), max = 400 mg/kg^[5] (s.c.)

给药途径
i.d., i.p., s.c.

动物药代数据
Animal Rats^[6]
Dose 9 mg/kg
Administration p.o.
T_max 1.5 h
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	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8577 mL
- 19.2886 mL
- 38.5773 mL
- 5 mM
- 0.7715 mL
- 3.8577 mL
- 7.7155 mL
- 10 mM
- 0.3858 mL
- 1.9289 mL
- 3.8577 mL

技术信息

CAS号

50924-49-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C9H13N3O6

运输

蓝冰

分子量

259.22

别名

NSC 289637;HE 69;β-Bredinin;beta-Bredinin;Bredinin;咪唑立宾

溶解度

DMSO	50.0 mg/mL (192.9 mM)
Water	50.0 mg/mL (192.9 mM)

动物实验配方

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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	-	-
NCT02005757	Rheumatoid Arthritis	Phase 2	Unknown	October 2016	Korea, Republic of ... more >> Hallym University Sacred Heart Hospital Recruiting Anyang, Korea, Republic of Contact: Young-Il Seo, PhD yiseo@hallym.or.kr Principal Investigator: Young-Il Seo, PhD Hallym University chuncheon Sacred Heart Hospital Recruiting Chuncheon, Korea, Republic of Contact: Kyeong Min Son, PhD jollyfox@hanmail.net Principal Investigator: Kyeong Min Son Eulji University Hospital Recruiting Daejeon, Korea, Republic of Contact: Donghyuk Sheen, PhD rheuma@eulji.ac.kr Principal Investigator: Donghyuk Sheen, PhD Gangneung Asan Hospital Recruiting Gangneung, Korea, Republic of Contact: Sung-Soo Kim, Ph.D 82-33-610-3061 drkiss@ulsan.ac.kr Principal Investigator: Sung-Soo Kim, Ph.D Kangwon National University Hospital Recruiting Kangwon, Korea, Republic of Contact: Kiwon Moon, PhD kiwonmoon@kangwon.ac.kr Principal Investigator: Kiwon Moon Kyung Hee University hospital Recruiting Seoul, Korea, Republic of Contact: Seung-Jae Hong, phD hsj718@khu.ac.kr Principal Investigator: Seung-Jae Hong, phD Soon Chun Hyang University Hospital Recruiting Seoul, Korea, Republic of Contact: Hyun-sook Kim, PhD healthyra@schmc.ac.kr Principal Investigator: Hyunsook Kim Collapse <<
NCT02373202	Rheumatoid Arthritis	Phase 3	Completed	-	Japan ... more >> Investigational Site Number 392010 Asahi-Shi, Japan Investigational Site Number 392001 Asahikawa-Shi, Japan Investigational Site Number 392070 Beppu-Shi, Japan Investigational Site Number 392036 Chiba-Shi, Japan Investigational Site Number 392083 Chuo-Ku, Japan Investigational Site Number 392004 Fukui-Shi, Japan Investigational Site Number 392039 Fukuoka-Shi, Japan Investigational Site Number 392030 Ichinomiya-Shi, Japan Investigational Site Number 392002 Iizuka-Shi, Japan Investigational Site Number 392019 Kagoshima-Shi, Japan Investigational Site Number 392066 Kamakura-Shi, Japan Investigational Site Number 392050 Kato-Shi, Japan Investigational Site Number 392037 Kawachi-Nagano-Shi, Japan Investigational Site Number 392099 Kawasaki-Shi, Japan Investigational Site Number 392013 Kitakyushu-Shi, Japan Investigational Site Number 392097 Kochi-Shi, Japan Investigational Site Number 392065 Kushiro-Shi, Japan Investigational Site Number 392026 Matsuyama-Shi, Japan Investigational Site Number 392034 Miyagi-Gun, Japan Investigational Site Number 392076 Nagoya-Shi, Japan Investigational Site Number 392080 Nagoya-Shi, Japan Investigational Site Number 392046 Narashino-Shi, Japan Investigational Site Number 392059 Oita-Shi, Japan Investigational Site Number 392062 Okayama-Shi, Japan Investigational Site Number 392027 Osaki-Shi, Japan Investigational Site Number 392049 Sagamihara-Shi, Japan Investigational Site Number 392014 Sapporo-Shi, Japan Investigational Site Number 392041 Sapporo-Shi, Japan Investigational Site Number 392073 Sapporo-Shi, Japan Investigational Site Number 392006 Sasebo-Shi, Japan Investigational Site Number 392021 Sendai-Shi, Japan Investigational Site Number 392022 Sendai-Shi, Japan Investigational Site Number 392033 Sendai-Shi, Japan Investigational Site Number 392071 Sendai-Shi, Japan Investigational Site Number 392029 Shizuoka-Shi, Japan Investigational Site Number 392023 Takaoka-Shi, Japan Investigational Site Number 392003 Tomakomai-Shi, Japan Investigational Site Number 392074 Urasoe-Shi, Japan Investigational Site Number 392079 Urayasu-Shi, Japan Investigational Site Number 392048 Yokohama-Shi, Japan Collapse <<

咪唑利宾 Catalog No. CSN11454

靶点选择性

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