| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 5g |
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| Targets |
Moroxydine is a broad-spectrum antiviral agent. [1]
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|---|---|
| ln Vitro |
In CIK cells infected with grass carp reovirus (GCRV), moroxydine (6.3 μg/mL for 96 h) prevented approximately 50% of virus-induced apoptosis. [1]
- Moroxydine (40 μg/mL) significantly inhibited GCRV-induced cytopathic effects (CPE) and cell death, maintaining normal cell morphology up to 96 h post-infection. [1] - Transmission electron microscopy showed that moroxydine treatment eliminated viral nucleocapsids in CIK cells and preserved normal ultrastructure, while untreated infected cells showed extensive vacuolation, karyolysis, and virion clusters. [1] - Moroxydine (20 μg/mL) significantly suppressed the expression of GCRV viral protein genes (vp1–vp4) in a time-dependent manner, with vp1 and vp2 showing the greatest inhibition. [1] - Moroxydine treatment (20 μg/mL) significantly reduced viral titer (ln TCID₅₀) at 12, 24, 48, and 72 h compared to untreated infected cells. [1] - Moroxydine prevented GCRV-induced downregulation of Bcl-2 and upregulation of Bax, as well as the activation of caspase-9 and caspase-3, as shown by Western blot and caspase activity assays. [1] - Flow cytometry analysis showed that moroxydine (40 μg/mL) significantly reduced the percentage of apoptotic cells induced by GCRV infection at 48 h. [1] - DNA fragmentation assays demonstrated that moroxydine protected CIK cells from GCRV-induced DNA damage. [1] |
| Enzyme Assay |
Caspase-3 activity was measured using a colorimetric activity assay kit with the chromogenic substrate Ac-DEVD-pNA. Cell lysates were incubated with the substrate at 37°C for 2 h, and absorbance was read at 405 nm. [1]
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| Cell Assay |
CIK cells (Ctenopharyngodon idella kidney) were cultured in MEM medium with 10% fetal calf serum at 28 ± 0.5°C. [1]
- Cytotoxicity assay: Cells were treated with moroxydine (15.6–1000 μg/mL) for 96 h, and cell viability was measured using WST-8 assay. TC₅₀ and safe concentration (SC) were calculated. [1] - Antiviral activity: Cells were infected with 100 TCID₅₀ GCRV for 2 h, then treated with moroxydine (1–100 μg/mL) for 24–96 h. Cell viability was assessed by WST-8 assay. [1] - Metabolism assay: CIK cells were exposed to moroxydine (218.5 μg/mL, SC) for 6 h, then medium was replaced with drug-free MEM every 2 h. Cells were harvested hourly, lysed, and moroxydine content was quantified by HPLC (210 nm, methanol:water 7:3). [1] - Morphological observation: Cells were observed under inverted microscope at 48 and 96 h post-treatment. Scanning and transmission electron microscopy were performed on samples fixed in 2.5% glutaraldehyde, dehydrated, and imaged. [1] - Apoptosis assays: DAPI and Dil staining for nuclear/cytoplasmic morphology; DNA fragmentation by agarose gel electrophoresis; flow cytometry with PI staining after ethanol fixation. [1] - Western blot: Cells lysed in RIPA buffer with PMSF; proteins separated by 12% SDS-PAGE, transferred to PVDF, probed with antibodies against Bcl-2, Bax, caspase-3, caspase-9, and β-actin, detected by HRP-DAB. [1] - RT-qPCR: RNA extracted with TRIzol, cDNA synthesized using oligo dT primers. qPCR performed for GCRV vp1–vp4 genes using SYBR Green. Fold changes calculated by ΔΔCt method. [1] |
| ADME/Pharmacokinetics |
In CIK cells, moroxydine reached maximum intracellular concentration after 4 h of exposure at the safe concentration (218.5 μg/mL), with a content of 16.7 ± 0.6 μg per 10⁶ cells. After removal of the drug, intracellular levels declined sharply, reaching a low level of 0.93 ± 0.15 μg per 10⁶ cells at 5 h post-removal. [1]
- HPLC analysis: retention time of moroxydine was approximately 3.86 min; linear regression equation: y = 0.044x + 0.52 (R² = 0.98). [1] |
| Toxicity/Toxicokinetics |
Moroxydine showed lower cytotoxicity than ribavirin. The 96 h half-toxic concentration (TC₅₀) was 1246.0 ± 9.5 μg/mL, and the safe concentration (SC) was 218.5 ± 32.0 μg/mL. [1]
- No significant cytotoxicity was observed at concentrations up to 250 μg/mL for 96 h. [1] - The safe concentration was approximately threefold higher than the effective concentration (40 μg/mL). [1] |
| References | |
| Additional Infomation |
Moroxydine hydrochloride is an antiviral agent discovered in the 1950s with activity against DNA and RNA viruses, including influenza, herpes simplex, varicella-zoster, measles, mumps, and hepatitis C virus. [1]
- This study is the first to report the anti-GCRV activity of moroxydine and its antiapoptotic mechanism in fish cells. [1] - Moroxydine inhibited viral replication by suppressing viral gene expression, particularly of vp1 (guanylyl transferase) and vp2 (RNA-dependent RNA polymerase), thereby preventing virus-induced apoptosis via the mitochondrial pathway. [1] - Moroxydine exhibited a good safety index (SC/EC ≈ 5.5) and rapid cellular metabolism, suggesting potential for use in aquaculture. [1] |
| Molecular Formula |
C6H13N5O
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|---|---|
| Molecular Weight |
171.2
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| Exact Mass |
207.088
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| CAS # |
3160-91-6
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| Related CAS # |
3160-91-6 (HCl);3731-59-7;
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| PubChem CID |
76621
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| Appearance |
White to off-white solid powder
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| Boiling Point |
327ºC at 760 mmHg
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| Melting Point |
211-214ºC(lit.)
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| Flash Point |
151.6ºC
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| LogP |
0.767
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
13
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| Complexity |
192
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1COCCN1C(=N)N=C(N)N.Cl
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| InChi Key |
FXYZDFSNBBOHTA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H13N5O.ClH/c7-5(8)10-6(9)11-1-3-12-4-2-11;/h1-4H2,(H5,7,8,9,10);1H
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| Chemical Name |
N-(diaminomethylidene)morpholine-4-carboximidamide;hydrochloride
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| Synonyms |
ABOBSKF 8898-AViruminWiruminBimolinMoroxydine free baseSKF 8898AVirugon
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
H2O : ≥ 100 mg/mL (~481.56 mM)
DMSO : ~50 mg/mL (~240.78 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (12.04 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 (12.04 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 (12.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (481.56 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.8411 mL | 29.2056 mL | 58.4112 mL | |
| 5 mM | 1.1682 mL | 5.8411 mL | 11.6822 mL | |
| 10 mM | 0.5841 mL | 2.9206 mL | 5.8411 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.
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