| CAS NO: | 50924-49-7 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| 1g | 电议 |
| 2g | 电议 |
| Molecular Weight (MW) | 259.22 |
|---|---|
| Formula | C9H13N3O6 |
| CAS No. | 50924-49-7 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: <1 mg/mL |
| Water: 52 mg/mL (200.6 mM) | |
| Ethanol: <1 mg/mL | |
| Solubility (In vivo) | Chemical Name: 1-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-5-hydroxy-1H-imidazole-4-carboxamide InChi Key: HZQDCMWJEBCWBR-UUOKFMHZSA-N InChi Code: InChI=1S/C9H13N3O6/c10-7(16)4-8(17)12(2-11-4)9-6(15)5(14)3(1-13)18-9/h2-3,5-6,9,13-15,17H,1H2,(H2,10,16)/t3-,5-,6-,9-/m1/s1 SMILES Code: O=C(C1=C(O)N([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)C=N1)N |
| Synonyms | HE 69; He69; NSC289637; NSC-289637; He-69; Mizoribine; Bredinin; NSC 289637. |
| In Vitro | In vitro activity: Mizoribine (1-50 mg/mL) is able to inhibit T cell proliferation by 10-100% in a dose-dependent fashion to all stimuli tested. Mizoribine leads to a decrease in intracellular GTP levels, and that repletion of GTP reversed its antiproliferative effects Mizoribine causes a dose-dependent inhibition of T cell proliferation, which is reversible with the addition of 50 mM guanosine to replete guanine ribonucleotide pools. Mizoribine selectively inhibits guanine ribonucleotide formation in purified T cells, whereas the effect of 6-mercaptopurine (6MP) appears to be more dependent on adenine ribonucleotide depletion. Mizoribine inhibits HCV RNA replication with IC50 of 100 μM. Cell Assay: Unlike azathioprine, Mizoribine is not taken up by nucleic acids in the cell. Instead, after phosphorylation MZR-5 -monophosphate inhibits GMP synthesis by the antagonistic blocking of IMPDH (Ki = 10(-8)M) and GMP- synthetase (Ki =10(-5) M). Pretreatment of cells with MZR partially, but significantly, attenuates the expression of monocyte chemoattractant protein (MCP)-1 mRNA and protein, whereas the poly IC-induced expressions for the other functional molecules, such as CCL5, fractalkine and IL-8 were not influenced by MZR treatment. |
|---|---|
| In Vivo | Mizoribine (5 or 10 mg/kg) suppresses urinary albumin excretion in the rats. Mizoribine (5 or 10 mg/kg) inhibits the development of glomerulosclerosis, interstitial fibrosis and macrophage infiltration in the kidney in the rats. Mizoribine (5 or 10 mg/kg) increases the expression of MCP-1, OPN and TGF-β1 mRNA in untreated OLETF rats. |
| Animal model | Rats |
| Formulation & Dosage | 5 or 10 mg/kg |
| References | Mol Pharmacol. 1992 Apr;41(4):671-6; Nephrol Dial Transplant. 2005 Aug;20(8):1573-81. |
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