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Purity: ≥98%
Mizoribine (also called Bredinin, HE-69; He69; NSC289637; NSC-289637) is an imidazole-based nucleoside isolated from the fungus Penicillium brefeldianum. It can be utilized as an immunosuppressive drug with an IC50 of 100 uM.
| Targets |
HCV; IMPDH; SARS-CoV
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| Cell Assay |
Mizoribine is not absorbed by the cell's nucleic acids, in contrast to azathioprine. Rather, MZR-5-monophosphate inhibits GMP synthesis by antagonistically blocking GMP synthetase (Ki = 10(-5) M) and IMPDH (Ki = 10(-8) M) following phosphorylation. Monocyte chemoattractant protein (MCP)-1 mRNA and protein expression is partially but significantly reduced when cells are pretreated with MZR; however, MZR treatment has no effect on the expressions of other functional molecules, such as CCL5, fractalkine, and IL-8, that are induced by polymer-coated capsules.
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| Animal Protocol |
Male DBA/1 J mice with collagen-induced arthritis
10, 20 and 50 mg/kg Administered orally 5 days a week for 12 weeks |
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| References |
| Molecular Formula |
C9H13N3O6
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| Molecular Weight |
259.22
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| Exact Mass |
259.08
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| Elemental Analysis |
C, 41.70; H, 5.05; N, 16.21; O, 37.03
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| CAS # |
50924-49-7
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| Appearance |
White solid powder
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| SMILES |
C1=NC(=C(N1[C@H]2[C@@H]([C@@H]([C@H](O2)CO)O)O)O)C(=O)N
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| InChi Key |
HZQDCMWJEBCWBR-UUOKFMHZSA-N
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| 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
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| Chemical Name |
1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-5-hydroxyimidazole-4-carboxamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06114953 | Recruiting | Drug: Mycophenolate Mofetil Drug: Mizoribine |
Kidney Transplant Immunosuppression |
Lee's Pharmaceutical Limited | January 1, 2023 | Phase 4 |
| NCT05293704 | Not yet recruiting | Drug: Mizoribine | Kidney Transplant Recipients BK Virus |
Lee's Pharmaceutical Limited | May 1, 2022 | Phase 4 |
| NCT02256150 | Completed | Drug: Cyclophosphamide (CTX) Drug: Mizoribine (MZR) |
Lupus Nephritis | Asahi Kasei Pharma Corporation | November 2014 | Phase 3 |
| NCT02257697 | Completed | Drug: Cyclophosphamide (CTX) Drug: Mizoribine (MZR) |
Nephrotic Syndrome | Asahi Kasei Pharma Corporation | November 2014 | Phase 3 |
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