product name Mizoribine
Description: Mizoribine (also known as Bredinin, NSC 289637) is a immunosuppressive agents (IC50=100 uM) that inhibit the proliferation of lymphocytes selectively, via inhibition of IMPDH. Mizoribine is an imidazole nucleoside, selectively inhibits inosine monophosphate synthetase and guanosine monophosphate synthetase. Mizoribine (1-50 mg/mL) is able to inhibit T cell proliferation by 10-100% in a dose-dependent fashion to all stimuli tested.
References: Mol Pharmacol. 1992 Apr;41(4):671-6; Nephrol Dial Transplant. 2005 Aug;20(8):1573-81.
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)
Synonyms
Bredinin, NSC 289637
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19412874
| 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. Kinase Assay: 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 | |
| Formulation & Dosage | |
| References | Mol Pharmacol. 1992 Apr;41(4):671-6; Nephrol Dial Transplant. 2005 Aug;20(8):1573-81. |
