| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
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| 2g |
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| 5g | |||
| 10g | |||
| Other Sizes |
| Targets |
Molsidomine is a prodrug that is metabolized to linsidomine (SIN-1), which releases nitric oxide (NO). NO activates soluble guanylate cyclase, leading to increased cGMP production, vasodilation, and reduced cardiac workload. It does not have a single protein target but acts through the NO-cGMP pathway.
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|---|---|
| ln Vitro |
Molsidomine is a prodrug that requires metabolic activation to release NO. Its in vitro activity is related to NO release and vasodilation. Specific IC50 values are not applicable as it acts through NO release rather than direct enzyme inhibition.
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| ln Vivo |
Molsidomine has been used clinically for the treatment of angina pectoris. It is a long-acting vasodilator that reduces cardiac preload and afterload, thereby decreasing myocardial oxygen demand. It has been shown to improve exercise tolerance in patients with angina.
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| Enzyme Assay |
In vitro assays for Molsidomine involve measuring the release of NO from its active metabolite SIN-1. NO release can be detected using chemiluminescence or Griess assay. Vasodilation can be assessed in isolated blood vessel preparations by measuring relaxation of pre-contracted vessels.
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| Cell Assay |
In vitro cell-based assays for Molsidomine assess its effects on NO production and cGMP accumulation in cultured cells. Cells are treated with Molsidomine or its active metabolite SIN-1, and NO levels or cGMP levels are measured. Vasodilation can be assessed in endothelial cell cultures.
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| Animal Protocol |
Molsidomine has been evaluated in animal models of angina and cardiovascular disease. It is typically administered orally, and its effects on hemodynamics, exercise tolerance, and myocardial ischemia are assessed. Clinical studies have also been conducted in patients with angina pectoris.
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| 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 Molsidomine is orally bioavailable and is rapidly absorbed from the gastrointestinal tract. It is metabolized in the liver to its active metabolite linsidomine (SIN-1). The half-life of Molsidomine is approximately 1-2 hours, while SIN-1 has a shorter half-life. It is excreted primarily in the urine. |
| Toxicity/Toxicokinetics |
Molsidomine is generally well-tolerated. Common side effects include headache, hypotension, and dizziness. It may cause tolerance with prolonged use. It is contraindicated in patients with severe hypotension, shock, or known hypersensitivity.
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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. Molsidomine is an FDA-approved drug for the treatment of angina pectoris. It is a long-acting vasodilator that acts through NO release. It is available in oral formulations for the prophylaxis and treatment of angina. It is also known by brand names such as Corvaton and Molsidolat. |
| Molecular Formula |
C9H14N4O4
|
|---|---|
| Molecular Weight |
242.23
|
| Exact Mass |
242.101
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| CAS # |
25717-80-0
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| PubChem CID |
5353788
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| Appearance |
White to off-white solid powder
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| Melting Point |
140-141°C
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| LogP |
2.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
17
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| Complexity |
270
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCO/C(=N/C1=C[N+](=NO1)N2CCOCC2)/[O-]
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| InChi Key |
XLFWDASMENKTKL-UHFFFAOYSA-N
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| 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
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| Synonyms |
N-(Ethoxycarbonyl)-3-(4-morpholinyl)sydnone imine Morsydomine SIN10 SIN-10 SIN 10Corvaton
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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 |
| 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) |
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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