| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
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| Targets |
Olprinone is a specific phosphodiesterase III (PDE3) inhibitor. PDE III is present in the myocardium, vascular smooth muscle, fat tissue, and platelets. Inhibition of PDE III enhances myocardial contraction, produces vasodilatation, and suppresses platelet aggregation. The PDE III isoenzyme is specific for cAMP and has no effect on cGMP and calmodulin. Therefore the inhibition of PDE III isoenzyme results in an increased level of cAMP. [2]
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| ln Vivo |
In rats with myocardial ischemia-reperfusion injury, olprinone (Loprinone) (0.2 mg/kg; intraperitoneal injection) reduces inflammation [1].
In a rat model of myocardial ischemia-reperfusion injury (25 min left anterior descending coronary artery occlusion followed by 1 h reperfusion), administration of Olprinone (0.2 mg/kg, i.p.) 15 min after ischemia significantly reduced: (1) histological evidence of myocardial injury (including reduced alteration of reticular fibers); (2) myocardial infarct size (expressed as a percentage of the area at risk); (3) elevation of serum lactate dehydrogenase (LDH) activity; (4) nuclear factor kappa-B (NF-κB) p65 expression in heart tissue; (5) pro-inflammatory cytokines: tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) immunostaining; (6) adhesion molecules: inter-cellular adhesion molecule 1 (ICAM-1) and P-selectin immunostaining; (7) nitrotyrosine formation; (8) poly(ADP-ribose) (PAR) formation (indicator of PARP activation); (9) apoptosis markers: Bax and Fas-L immunostaining, and TUNEL-positive apoptotic cells; and attenuated the loss of Bcl-2 immunostaining. [2] |
| Animal Protocol |
Animal/Disease Models: Male adult Wistar rat (250-300 g) (ischemia-reperfusion rat) [1]
Doses: 0.2 mg/kg Route of Administration: IP (administered 15 minutes after ischemia) Experimental Results:Dramatically diminished: (1) Histological evidence of myocardial injury, (2) Proinflammatory cytokines: tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β), (3) Adhesion molecules: intercellular adhesion molecules 1 (ICAM-1) and P-selectin, (4) nitrotyrosine formation, (5) nuclear factor kappa-B (NF-κB) expression, (6) poly(ADP-ribose) (PAR) formation , and (7) apoptosis (Bax, Bcl-2, Fas-L, and terminal deoxynucleotidyl transferase-mediated UTP end labeling (TUNEL). - Myocardial ischemia-reperfusion injury model in rats: Male adult Wistar rats (250-300 g) were anesthetized with thiopentone sodium (120 mg/kg i.p.). The trachea was cannulated, and animals were ventilated (inspiratory oxygen concentration: 30%; 70 strokes/min, tidal volume: 8-10 ml/kg). Body temperature was maintained at 37±1°C. A thoracotomy at the fifth left intercostal space was performed, the pericardium opened, and a loose 00 braided silk suture was placed around the left anterior descending coronary artery approximately 1-2 mm below its origin. A small silicon ring was inserted in the silk thread below the knot. The chest was closed, and rats were allowed to equilibrate for 20 min. Ischemia was induced by tightening the threads for 25 min. Reperfusion (1 h) was obtained by reopening the chest and cutting the ligature. Olprinone (0.2 mg/kg, i.p.) was administered 15 min after ischemia. At the end of the 1-h reperfusion, the LAD was recollected, and 1 mL of Evans blue dye (2% wt/vol) was injected via the jugular vein. The heart was excised, sectioned, and the area at risk (AAR) separated from nonischemic tissue. Infarct size was determined by incubation with p-nitroblue tetrazolium (0.5 mg/ml) for 30 min at 37°C. [2] - Sham-operated groups: Rats were subjected to identical surgical procedures except for coronary artery occlusion and were kept under anesthesia for the duration of the experiment. Sham + Olprinone group received olprinone (0.2 mg/kg i.p.) 15 min after the sham procedure. [2] |
| References |
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| Additional Infomation |
Olprinone belongs to the bipyridine class of compounds.
- Mechanism of action: Olprinone inhibits phosphodiesterase III, leading to increased cAMP levels. cAMP acts as a second messenger for a variety of hormones, inflammatory mediators and cytokines, and is part of an endogenous mechanism for down-regulating the inflammatory response. [2] - Therapeutic potential: The study provides evidence that treatment with Olprinone ameliorated the inflammatory process associated with myocardial ischemia-reperfusion in rats and suggests that this drug may have potential in the treatment of various ischemia and reperfusion diseases. [2] - Previous findings: Olprinone selectively improves carotid artery distensibility. Its anti-inflammatory effects have been previously demonstrated in ischemia-reperfusion-induced acute renal injury, lipopolysaccharide-induced lung injury, and endotoxic shock. [2] |
| Molecular Formula |
C14H10N4O
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|---|---|
| Molecular Weight |
250.2554
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| Exact Mass |
250.085
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| CAS # |
106730-54-5
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| Related CAS # |
Olprinone Hydrochloride;119615-63-3
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| PubChem CID |
4593
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Melting Point |
>300ºC
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| Index of Refraction |
1.703
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| LogP |
1.03
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
525
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JPAWFIIYTJQOKW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H10N4O/c1-9-12(6-11(7-15)14(19)17-9)10-2-3-13-16-4-5-18(13)8-10/h2-6,8H,1H3,(H,17,19)
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| Chemical Name |
5-imidazo[1,2-a]pyridin-6-yl-6-methyl-2-oxo-1H-pyridine-3-carbonitrile
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9958 mL | 19.9792 mL | 39.9584 mL | |
| 5 mM | 0.7992 mL | 3.9958 mL | 7.9917 mL | |
| 10 mM | 0.3996 mL | 1.9979 mL | 3.9958 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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