[CAS NO. 50924-49-7]  Mizoribine

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PRODUCTS SPECIFICATIONS [50924-49-7]

Catalog
HY-17470
Brand
MCE
CAS
50924-49-7

DESCRIPTION [50924-49-7]

Overview

MDLMFCD00057221
Molecular Weight259.22
Molecular FormulaC9H13N3O6
SMILESOC[C@@H]1[C@@H](O)[C@@H](O)[C@H](N2C(O)=C(C(N)=O)N=C2)O1

For research use only. We do not sell to patients.


Summary

Mizoribine (NSC 289637), an imidazole nucleoside, inhibits HCV RNA replication with IC 50 of approximately 100 μM for anti-HCV activity. Immunosuppressant [1] . Mizoribine, an IMPDH inhibitor, inhibits replication of SARS-CoV with IC 50 s of 3.5 μg/mL and 16 μg/mL for SARS-CoV Frankfurt-1 and SARS-CoV HKU39849, respectively [2] .


IC50 & Target

HCV [1] ; IMPDH; SARS-CoV [2]


In Vitro

Mizoribine, isolated from culture medium of the mold Eupenicillium brefeldianum M-2166, acts as an immunosuppressant which exerts its effects without severe side effects [1] .
Mizoribine is an inosine-5′-monophosphate dehydrogenase (IMPDH) inhibitorused for renal transplantation, autoimmune diseases and steroid-resistant nephrotic syndrome [2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.


In Vivo

Mizoribine suppresses collagen-induced arthritis. Mizoribine (10, 20 and 50 mg/kg; Administered orally 5 days a week for 12 weeks) reduces the arthritis score in a dose-dependent fashion, showing significant suppression, even at a dose of 10 mg/kg [3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male DBA/1 J mice with collagen-induced arthritis [3]
Dosage: 10, 20 and 50 mg/kg
Administration: Administered orally 5 days a week for 12 weeks
Result: Showed dose-dependency of the suppressive effect.

Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT02373202 Sanofi|Regeneron Pharmaceuticals
Rheumatoid Arthritis
February 2015 Phase 3
NCT02257697 Asahi Kasei Pharma Corporation
Nephrotic Syndrome
November 2014 Phase 3
NCT02256150 Asahi Kasei Pharma Corporation
Lupus Nephritis
November 2014 Phase 3

Appearance

Solid


Source

Eupenicillium brefeldianum M-2166


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL ( 482.22 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8577 mL 19.2886 mL 38.5773 mL
5 mM 0.7715 mL 3.8577 mL 7.7155 mL
10 mM 0.3858 mL 1.9289 mL 3.8577 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution

  • 2.

    Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution

  • 3.

    Add each solvent one by one: 10% DMSO >> 90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.64 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

1H-Imidazole-4-carboxamide, 5-hydroxy-1-β-D-ribofuranosyl-
5-Hydroxy-1-β-D-ribofuranosyl-1H-imidazole-4-carboxamide
Bredinin
Mizoribine
β-Bredinin
HE 69
NSC 289637