Mizoribine

Catalog No.S1384 Synonyms: Bredinin, NSC 289637

Mizoribine  Chemical Structure

Molecular Weight(MW): 259.22

Mizoribine is an imidazole nucleoside, selectively inhibits inosine monophosphate synthetase and guanosine monophosphate synthetase.

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Biological Activity

Description Mizoribine is an imidazole nucleoside, selectively inhibits inosine monophosphate synthetase and guanosine monophosphate synthetase.
Targets
Monophosphate synthetase [2]
In vitro

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. [1] 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. [2] Mizoribine inhibits HCV RNA replication with IC50 of 100 μM. [3]

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. [4]

Protocol

Solubility (25°C)

In vitro Water 51 mg/mL (196.74 mM)
DMSO 1 mg/mL (3.85 mM)
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 259.22
Formula

C9H13N3O6

CAS No. 50924-49-7
Storage powder
in solvent
Synonyms Bredinin, NSC 289637

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02373202 Completed Rheumatoid Arthritis Sanofi|Regeneron Pharmaceuticals February 2015 Phase 3
NCT02373202 Completed Rheumatoid Arthritis Sanofi|Regeneron Pharmaceuticals February 2015 Phase 3
NCT02256150 Active not recruiting Lupus Nephritis Asahi Kasei Pharma Corporation November 2014 Phase 3
NCT02257697 Completed Nephrotic Syndrome Asahi Kasei Pharma Corporation November 2014 Phase 3
NCT02256150 Active not recruiting Lupus Nephritis Asahi Kasei Pharma Corporation November 2014 Phase 3
NCT02257697 Completed Nephrotic Syndrome Asahi Kasei Pharma Corporation November 2014 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID