Cas No.: | 50924-49-7 |
Chemical Name: | Mizoribine |
Synonyms: | Mizoribine;N'-[BETA-D-RIBOFURANOSYL]-5-HYDROXYIMIDAZOLE-4-CARBOXAMIDE;4-carbamoyl-1-beta-d-ribofuranosyl-imidazolium-5-olate;5-hydroxy-1-beta-d-ribofuranosyl-1h-imidazole-4-carboxamid;anhydro-4-carbamoyl-5-hydroxy-1-beta-d-ribofuranosyl-imidazoliumhydroxide;bredinin;bredinine;n'-(β-d-ribofuranosyl)-5-hydroxy-imida-zole-4-carboxamide;1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-hydroxyimidazole-4-carboxamide;1H-Imidazole-4-carboxamide, 5-hydroxy-1-β-D-ribofuranosyl-;1-(β-D-Ribofuranosyl)-5-hydroxyimidazole-4-carboxamide;HE 69;HE-69;Mizoribina;Mizoribina [INN-Spanish];Mizoribine [INN:JAN];Mizoribinum;Mizoribinum [INN-Latin];NSC 289637;N′-(β-D-Ribofuranosyl)-5-hydroxyimidazole-4-carboxamide;5-Hydroxy-1-beta-D-ribofuranosyl-1H-imidazole-4-carboxamide |
SMILES: | O=C(C1=C(O)N([C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)C=N1)N |
Formula: | C9H13N3O6 |
M.Wt: | 259.216022253037 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | Mizoribine(NSC 289637; HE 69; β-Bredinin) is an immunosuppressive agents (IC50=100 uM) that inhibit the proliferation of lymphocytes selectively, via inhibition of IMPDH.IC50 Value:Target: IMPDHin vitro: 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) [1]. 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 [2].in vivo:MZR 150 mg was administered once a day. After 6 months, the remission rate was 72.7% (2 subjects achieved complete remission, and 9 partial remission). After 3 and 6 months, significant reductions (p < 0.01) were obtained in 24-h proteinuria (g/day) [3]. |
References: | [1]. Ishikawa H. Mizoribine and mycophenolate mofetil. Curr Med Chem. 1999 Jul;6(7):575-97. [2]. Aizawa T, et al. Mizoribine selectively attenuates monocyte chemoattractant protein-1 production in cultured human glomerular mesangial cell: A possible benefit of its use in the treatment of lupus nephritis. Nephrology (Carlton). 2014 Jan;19(1):47-52. [3]. Zhang M, et al. Study of the efficacy of mizoribine in lupus nephritis in Chinese patients. Rheumatol Int. 2013 Nov;33(11):2737-42. |