Mizoribine

Mizoribine is an imidazole nucleoside with immunosuppressive properties. It inhibits T cell proliferation in response to various mitogenic stimuli by 10-100% when used at concentrations ranging from 1 to 50 µg/mL. Mizoribine inhibits proliferation of stimulated T cells (IC50 = 5 µg/ml), which can be reversed by guanosine. It also inhibits guanine nucleotide formation in T cells, reducing GTP pools by 40-60% when used at a concentration of 5 µg/ml. Mizoribine inhibits replication of hepatitis C virus (HCV) RNA in vitro (IC50 = 100 µM). It suppresses glomerulosclerosis, urinary albumin excretion, interstitial fibrotic lesions, and macrophage infiltration into glomeruli and the interstitium in a rat model of type 2 diabetes when used at doses of 5 or 10 mg/kg. Mizoribine also reduces MCP-1, osteopontin (OPN), and TGF-beta1 mRNA expression in the kidney in the same model. Formulations containing mizoribine have been used for the prevention of rejection after renal transplantation as well as in the treatment of lupus nephritis, rheumatoid arthritis, and primary nephritic syndrome.Formal Name: 5-hydroxy-1-beta-D-ribofuranosyl-1H-imidazole-4-carboxamide. CAS Number: 50924-49-7. Synonyms: NSC 289637. Molecular Formula: C9H13N3O6. Formula Weight: 259.2. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: Soluble. lambdamax: 242, 285 nm. SMILES: OC[C@@H]1[C@@H](O)[C@@H](O)[C@H](N2C=NC(C(N)=O)=C2O)O1. 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. InChi Key: HZQDCMWJEBCWBR-UUOKFMHZSA-N.