| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Revizinone targets phosphodiesterase (PDE) III, an enzyme that hydrolyzes cyclic nucleotides (cAMP and cGMP) and plays a critical role in regulating intracellular signaling pathways. PDE III is involved in various physiological processes, including cardiac contractility, platelet aggregation, and smooth muscle relaxation. Revizinone is a selective PDE III inhibitor with an IC50 of 0.036 µM in enzyme assays. By inhibiting PDE III, Revizinone increases intracellular cAMP and cGMP levels, thereby modulating downstream signaling pathways.
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| ln Vitro |
In vitro, Revizinone is a selective PDE III inhibitor with an IC50 of 0.036 µM in enzyme assays. It inhibits cyclic nucleotide phosphodiesterase type III. Its activity is typically measured using enzyme assays with purified PDE III and a substrate. The compound's selectivity for PDE III over other PDE isoforms has been confirmed, though specific selectivity data is not detailed in standard product descriptions. These in vitro studies establish Revizinone as a potent and selective PDE III inhibitor.
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| ln Vivo |
In vivo activity data for Revizinone is limited, as the compound is primarily used as a research tool in in vitro studies. However, as a PDE III inhibitor, it may have effects on cardiac contractility, platelet aggregation, and smooth muscle relaxation. Specific in vivo protocols and results are not detailed in standard product descriptions. Its use is limited to research applications to study the role of PDE III in various physiological and pathological processes.
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| Enzyme Assay |
In vitro enzyme assays for Revizinone measure its inhibition of PDE III activity. PDE III enzyme is incubated with a substrate (e.g., cAMP or cGMP) in the presence of varying concentrations of Revizinone. The hydrolysis of the substrate is measured, and the IC50 is determined from the dose-response curve. For Revizinone, the IC50 is 0.036 µM. Selectivity is assessed by testing the compound against other PDE isoforms (PDE I, II, IV, V, etc.) to confirm its specificity for PDE III.
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| Cell Assay |
In vitro cell-based assays for Revizinone are used to study its effects on cyclic nucleotide signaling in relevant cell types. Cells (e.g., cardiac myocytes, platelets, or smooth muscle cells) are treated with Revizinone at various concentrations, and the levels of cAMP and cGMP are measured by ELISA or RIA. The compound's effects on cell function, such as platelet aggregation or smooth muscle contraction, can also be assessed. These cell-based assays confirm the biological activity of Revizinone as a PDE III inhibitor.
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| Animal Protocol |
In vivo animal experiments for Revizinone are not extensively described in the available literature. As a research compound, its use in vivo would be determined by the specific research question being addressed. A typical protocol for studying a PDE III inhibitor would involve its administration to animal models of cardiovascular or other diseases, with endpoints such as hemodynamic measurements, platelet function, or smooth muscle relaxation. However, specific protocols for Revizinone are not detailed.
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| ADME/Pharmacokinetics |
Revizinone has a molecular weight of 459.54 g/mol and a molecular formula of C26H29N5O3. It is a solid compound. It is soluble in DMSO and other organic solvents. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. As a research compound, its stability is maintained by proper storage as a dry powder.
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| Toxicity/Toxicokinetics |
Detailed toxicity data for Revizinone is not provided in standard product descriptions. As a research compound, its toxicity profile has not been extensively characterized. Revizinone is a PDE III inhibitor, and its toxicity would be related to its effects on PDE III-mediated signaling in normal tissues. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling Revizinone. Its use is limited to research applications and it is not intended for human or veterinary use.
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| References |
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| Additional Infomation |
Revizinone (R80122) is a research compound and is not approved for any clinical or therapeutic use. It is a new selective phosphodiesterase (PDE) III inhibitor with an IC50 of 0.036 µM in enzyme assays. Revizinone inhibits cyclic nucleotide phosphodiesterase type III. The compound is a research tool for studying the role of PDE III in various physiological processes, including cardiac contractility, platelet aggregation, and smooth muscle relaxation. Its mechanism of action involves inhibiting PDE III, thereby increasing intracellular cAMP and cGMP levels.
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| Molecular Formula |
C26H29N5O3
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| Molecular Weight |
459.55
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| Exact Mass |
459.227
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| CAS # |
133718-29-3
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| Related CAS # |
R 80123;133718-30-6
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| PubChem CID |
135544124
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| Appearance |
White to off-white solid powder
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| Density |
1.336g/cm3
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| Boiling Point |
627.743ºC at 760 mmHg
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| Flash Point |
333.447ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.677
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| LogP |
2.881
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
815
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C1CCCCC1)C(=O)CO/N=C(\C2=CC=CC=C2)/C3=CC4=C(C=C3)N=C5NC(=O)CN5C4
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| InChi Key |
VHDUUXNHZLBGHQ-XLVZBRSZSA-N
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| InChi Code |
InChI=1S/C26H29N5O3/c1-30(21-10-6-3-7-11-21)24(33)17-34-29-25(18-8-4-2-5-9-18)19-12-13-22-20(14-19)15-31-16-23(32)28-26(31)27-22/h2,4-5,8-9,12-14,21H,3,6-7,10-11,15-17H2,1H3,(H,27,28,32)/b29-25+
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| Chemical Name |
N-cyclohexyl-N-methyl-2-[(E)-[(2-oxo-3,5-dihydro-1H-imidazo[2,1-b]quinazolin-7-yl)-phenylmethylidene]amino]oxyacetamide
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| Synonyms |
R80123 R-80123 R 80123
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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 : ≥ 4.6 mg/mL (~10.01 mM)
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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 | 2.1760 mL | 10.8802 mL | 21.7604 mL | |
| 5 mM | 0.4352 mL | 2.1760 mL | 4.3521 mL | |
| 10 mM | 0.2176 mL | 1.0880 mL | 2.1760 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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