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Mizoribine

Cat. No. M1921
Mizoribine Structure
Synonym:

Bredinin

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
5mg USD 35  USD35 In stock
10mg USD 50  USD50 In stock
50mg USD 115  USD115 In stock
100mg USD 195  USD195 In stock
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Quality Control & Documentation
Biological Activity

Mizoribine is a newly developed immunosuppressive agent that has low toxicity. Mizoribine (Bredinin) exerts its activity through selective inhibition of inosine monophosphate synthetase and guanosine monophosphate synthetase, resulting in the complete inhibition of guanine nucleotide synthesis without incorporation into nucleotides. It arrests DNA synthesis in the S phase of cellular division. Mizoribine has a therapeutic role in some patients with chronic autoimmune urticaria and may be useful for treatment of cases not responsive to classical therapy. In vitro basophil histamine release assays suggested that Mizoribine might help to reduce anti-IgE autoantibody acting on the surface of basophils in chronic autoimmune urticaria. Mizoribine (MZR) reduced PAN-induced integrin-linked kinase activation (ILK) and phosphorylation of glycogen synthase kinase-3beta (GSK3beta) in vivo and in vitro. Mizoribine (MZR) directly prevents PAN-induced podocyte injury, possibly by affecting signaling cascades involving ILK and GSK3beta.

Chemical Information
Molecular Weight 259.22
Formula C9H13N3O6
CAS Number 50924-49-7
Solubility (25°C) Water ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Hashimoto T, et al. Dermatol Ther. Mizoribine treatment for antihistamine-resistant chronic autoimmune urticaria.

[2] Takeuchi S, et al. Nephron Exp Nephrol. The immunosuppressive drug mizoribine directly prevents podocyte injury in puromycin aminonucleoside nephrosis.

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