| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 2g |
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| 5g | |||
| 10g | |||
| Other Sizes |
Molsidomine is an orally bioactive and long acting vasodilator acting as an NO donor and annexin A2 inhibitor. It is metabolized in the liver to the active metabolite linsidomine, which is an unstable compound that releases nitric oxide (NO) upon decay as the actual vasodilating compound. It inhibits PDGF-induced smooth muscle cell migration, suppresses carotid artery neointima formation, and prevents activated platelet adhesion.
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Peak plasma concentration (tmax) is reached 1 to 2 hours after administration. Renal excretion is the primary route of elimination for metabolites in the human body (90% to 95%). Approximately 2% of ingested drugs are excreted unchanged in the urine. Metabolism/Metabolites Moxidamine is metabolized in the liver to lixidamine. Lixidamine decays by releasing nitric oxide (NO) from endothelial cells, which acts as the active vasodilator metabolite responsible for moxidamine's pharmacological action. The oral absorption rate of moxidamine is 95.5% ± 4.5%. The first-pass metabolism rate is 56%, and extensive hepatic metabolism has been reported. Renal excretion accounts for 95%, and the plasma half-life is 5 hours. Back to Top |
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| Additional Infomation |
1-Ethoxy-N-[3-(4-morpholino)-5-oxadiazol-3-onyl]methylimine ester belongs to the morpholino group of compounds. Moxidomin is an orally effective, long-acting vasodilator belonging to the synthetic ketone class of drugs. Interestingly, it is being investigated as a preventative measure against cerebral infarction. A morpholino synthetic ketimine ethyl ester, in which the ketone oxygen atom is replaced by a nitrogen atom. It acts as a nitric oxide donor and is a vasodilator already used to treat angina.
Drug Indications Moxidomin's indications include ischemic heart disease, angina, chronic heart failure, and pulmonary hypertension. Mechanism of Action Moxidomin is a cardiovascular drug with a mechanism of action similar to that of organic nitrates. The metabolite SIN-1A of moxidomin contains a pharmacologically active nitric oxide group, which can increase cyclic guanosine monophosphate (cGMP) levels and decrease intracellular calcium ion concentration in smooth muscle cells. This leads to relaxation of vascular smooth muscle and inhibition of platelet aggregation. |
| Molecular Formula |
C9H14N4O4
|
|---|---|
| Molecular Weight |
242.23
|
| Exact Mass |
242.101
|
| CAS # |
25717-80-0
|
| PubChem CID |
5353788
|
| Appearance |
White to off-white solid powder
|
| Melting Point |
140-141°C
|
| LogP |
2.2
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
4
|
| Heavy Atom Count |
17
|
| Complexity |
270
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCO/C(=N/C1=C[N+](=NO1)N2CCOCC2)/[O-]
|
| InChi Key |
XLFWDASMENKTKL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C9H14N4O4/c1-2-16-9(14)10-8-7-13(11-17-8)12-3-5-15-6-4-12/h7H,2-6H2,1H3
|
| Chemical Name |
(1E)-1-ethoxy-N-(3-morpholin-4-yloxadiazol-3-ium-5-yl)methanimidate
|
| Synonyms |
N-(Ethoxycarbonyl)-3-(4-morpholinyl)sydnone imine Morsydomine SIN10 SIN-10 SIN 10Corvaton
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ≥ 100 mg/mL (~412.83 mM)
H2O : ~25 mg/mL (~103.21 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.32 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 (10.32 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 (10.32 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: 25 mg/mL (103.21 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 | 4.1283 mL | 20.6415 mL | 41.2831 mL | |
| 5 mM | 0.8257 mL | 4.1283 mL | 8.2566 mL | |
| 10 mM | 0.4128 mL | 2.0642 mL | 4.1283 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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