| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| Other Sizes |
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| ln Vitro |
In vitro and ex vivo, amrinone (Inamrinone) exhibits fold suppression of ADP-induced ischemia aggregation in spots. Amrinone also reduced ischemia in human aortic smooth muscle cells activated by FBS or PDGF culture [4].
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|---|---|
| ln Vivo |
Amrinone (Inamrinone) was injected subcutaneously for 14 days at a dose of 10 mg/kg/day for support, and a substantial reduction in neointimal thickness was seen [4].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
The primary route of excretion in man is via the urine as both inamrinone and several metabolites (N-glycolyl, N-acetate, O-glucuronide and N-glucuronide). 1.2 L/kg [normal volunteers] Metabolism / Metabolites Hepatic. Biological Half-Life 5 to 8 hours |
| Toxicity/Toxicokinetics |
Protein Binding
10 to 49% |
| References |
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| Additional Infomation |
Amrinone is a 3,4'-bipyridine substituted at positions 5 and 6 by an amino group and a keto function respectively. A pyridine phosphodiesterase 3 inhibitor, it is a drug that may improve the prognosis in patients with congestive heart failure. It has a role as an EC 3.1.4.* (phosphoric diester hydrolase) inhibitor and a cardiovascular drug.
Amrinone (or inamrinone) is a type 3 pyridine phosphodiesterase inhibitor. It is used in the treatment of congestive heart failure. Inamrinone is a synthetic bipyridine phosphodiesterase inhibitor with inotropic and vasodilator properties. Inamrinone inhibits type III phosphodiesterase, which is abundant in cardiac and vascular tissues, thereby preventing the degradation of cyclic adenosine monophosphate (cAMP) and increasing intracellular concentrations of this secondary messenger. Elevated levels of cAMP increase the contractile force of the cardiac muscle and produce positive inotropic effects. Although the mechanism of action is not fully understood, inamrinone causes smooth muscle relaxation, resulting in peripheral vasodilation (reduced afterload) and a decreased pulmonary vascular resistance (reduced preload). A positive inotropic cardiotonic (CARDIOTONIC AGENTS) with vasodilator properties, phosphodiesterase 3 inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell. Drug Indication Used in the treatment of congestive heart failure. Mechanism of Action Amrinone is a phosphodiesterase inhibitor (PDE3), resulting in increased cAMP and cGMP which leads to an increase in the calcium influx like that caused by beta-agonists resulting in increased inotropic effect. Pharmacodynamics Amrinone is a positive inotropic cardiotonic with vasodilator properties, phosphodiesterase inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell. |
| Molecular Formula |
C10H9N3O
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|---|---|
| Molecular Weight |
187.1980
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| Exact Mass |
187.074
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| CAS # |
60719-84-8
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| Related CAS # |
60719-84-8 (free); 75898-90-7 (lactate);
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| PubChem CID |
3698
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
451.5±45.0 °C at 760 mmHg
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| Melting Point |
294-297ºC
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| Flash Point |
226.9±28.7 °C
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| Vapour Pressure |
0.0±1.1 mmHg at 25°C
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| Index of Refraction |
1.625
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| LogP |
-0.54
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
14
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| Complexity |
301
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RNLQIBCLLYYYFJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H9N3O/c11-9-5-8(6-13-10(9)14)7-1-3-12-4-2-7/h1-6H,11H2,(H,13,14)
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| Chemical Name |
3-amino-5-pyridin-4-yl-1H-pyridin-2-one
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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 : ~16.67 mg/mL (~89.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (8.92 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 16.7 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.3419 mL | 26.7094 mL | 53.4188 mL | |
| 5 mM | 1.0684 mL | 5.3419 mL | 10.6838 mL | |
| 10 mM | 0.5342 mL | 2.6709 mL | 5.3419 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 |
| NCT00060840 | Completed | Drug: Nitric Oxide Drug: Nitrogen |
Congestive Heart Failure | Mallinckrodt | 2003-07 | Phase 2 |
| NCT02174029 | Completed | Procedure: Ventilation- mandatory Procedure: Ventilation- voluntary mode only Procedure: Voluntary with preceding mandatory |
Muscle Atrophy or Weakness Ventilator-associated Lung Injury |
Steve Reynolds | 2014-06 | |
| NCT05011617 | Completed | Device: Non-intubation and monitoring anesthesia care (MAC) | Cardiac Surgery Monitored Anesthesia Care Postoperative Recovery |
ShuGuang Hospital | 2012-04-01 | Not Applicable |
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