| Description | Mizoribine (NSC-289637) belongs to the family of 1-Ribosyl-imidazolecarboxamides. Mizoribine has been investigated for the treatment of Rheumatoid Arthritis. |
| In vitro | Mizoribine选择性抑制纯化T细胞中的鸟嘌呤核糖核苷酸形成,而6-巯基嘌呤（6MP）的作用似乎更依赖于腺嘌呤核糖核苷酸消耗。1-50 mg/mL Mizoribine能够以剂量依赖性方式抑制所有测试刺激的T细胞增殖10-100％。Mizoribine剂量依赖性抑制T细胞增殖,在加入50 mM鸟苷到充满鸟嘌呤的核苷酸池时,该抑制作用是可逆的。Mizoribine抑制HCV RNA复制,IC50值为100 μM。Mizoribine导致细胞内GTP水平降低,并且GTP的补充逆转其抗增殖作用。 |
| In vivo | 5或10 mg/kg Mizoribine增加MCP-1,OPN以及TGF-β1 mRNA在未处理OLETF大鼠体内的表达.5或10 mg/kg Mizoribine抑制大鼠体内尿白蛋白排泄.5或10 mg/kg Mizoribine在大鼠肾脏中抑制肾小球硬化症,肾间质纤维化和巨噬细胞浸润的发展. |
| Target activity | Immunosuppressive:100 μM |
| Synonyms | Bredinin, NSC 289637, 咪唑立宾, HE 69 |
| molecular weight | 259.22 |
| Molecular formula | C9H13N3O6 |
| CAS | 50924-49-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (231.46 mM) Ethanol: < 1 mg/mL (insoluble or slightly soluble) H2O: 47 mg/mL (181.3 mM) |
| References | 1. Turka LA, et al. J Clin Invest, 1991, 87(3), 940-948. 2. Dayton JS, et al. Mol Pharmacol, 1992, 41(4), 671-676. 3. Naka K, et al. Biochem Biophys Res Commun, 2005, 330(3), 871-879. 4. Kikuchi Y, et al. Nephrol Dial Transplant, 2005, 20(8), 1573-1581. |