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| 25mg |
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Purity: ≥98%
| Targets |
WAY127093B racemate functions as a phosphodiesterase IV (PDE4) inhibitor. PDE4 is a key enzyme responsible for the hydrolysis of cyclic adenosine monophosphate (cAMP) in immune and inflammatory cells. By inhibiting PDE4, the compound prevents the breakdown of cAMP, leading to elevated intracellular cAMP levels, which in turn modulates the activity of protein kinase A and ultimately suppresses the production of pro-inflammatory cytokines, such as TNF-α, IL-2, and IFN-γ.
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| ln Vitro |
WAY127093B, the active enantiomer in the racemate, has shown potent PDE4 inhibitory activity in enzymatic assays. While specific IC50 values for the racemate are not detailed in standard summaries, the compound is described as a potent inhibitor. The racemate exhibits oral bioavailability and efficacy in preclinical models. In vitro assays typically measure the compound's ability to inhibit recombinant PDE4 activity and suppress LPS-induced TNF-α production in human peripheral blood mononuclear cells (PBMCs) or whole blood.
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| ln Vivo |
In guinea pig and rat models, WAY127093B demonstrates anti-inflammatory activity following oral administration. The compound's oral bioavailability supports its use in these in vivo efficacy studies. Specific in vivo data, such as ED50 values for inhibition of airway inflammation or other inflammatory endpoints, are not provided in the available summaries. However, its characterization as an orally active PDE4 inhibitor indicates that it has been evaluated in standard models of inflammation, such as LPS-induced pulmonary neutrophilia or antigen-induced airway hyperresponsiveness.
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| Enzyme Assay |
A typical protocol for evaluating PDE4 inhibition begins with preparing a dilution series of the test compound in a suitable buffer (e.g., 50 mM Tris-HCl, pH 7.5, containing 1 mM MgCl2, 0.05% BSA, and 0.5 mM cAMP). The compound is incubated with a source of PDE4 enzyme (recombinant or tissue homogenate) at 30°C for 20 minutes. The reaction is initiated by adding [³H]-cAMP. After incubation, the reaction is terminated by boiling, and the [³H]-AMP produced is converted to [³H]-adenosine by adding snake venom 5'-nucleotidase. The product is then separated using ion-exchange resin, and radioactivity is measured by scintillation counting. IC50 values are calculated from inhibition curves.
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| Cell Assay |
For evaluating the cellular activity of PDE4 inhibitors, human peripheral blood mononuclear cells (PBMCs) are isolated from healthy donors using Ficoll-Paque density gradient centrifugation. Cells are plated in 96-well plates and pre-incubated with varying concentrations of the test compound for 30-60 minutes. Cells are then stimulated with lipopolysaccharide (LPS, e.g., 1 µg/mL) for 18-24 hours to induce cytokine production. Supernatants are collected, and levels of pro-inflammatory cytokines such as TNF-α and IL-2 are measured using ELISA. The compound's efficacy is reported as the IC50 for inhibition of cytokine production. Cytotoxicity is assessed using an MTT or LDH assay.
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| Animal Protocol |
Male Sprague-Dawley rats or Hartley guinea pigs are orally administered the test compound suspended in a vehicle (e.g., 0.5% methylcellulose) at doses ranging from 0.3 to 10 mg/kg. Following a predetermined time (e.g., 1 hour), animals are challenged with an inflammatory stimulus, such as intratracheal LPS instillation. After the challenge period (e.g., 4-6 hours), animals are euthanized, and bronchoalveolar lavage fluid (BALF) is collected. The BALF is analyzed for total and differential cell counts (neutrophils) and cytokine levels. Efficacy is expressed as the percentage inhibition of neutrophil influx or cytokine production relative to vehicle-treated controls.
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| ADME/Pharmacokinetics |
WAY127093B racemate is characterized as being orally bioavailable. While specific pharmacokinetic parameters (e.g., Cmax, Tmax, half-life, AUC) are not detailed in the available literature, its oral bioavailability in guinea pigs and rats is a key feature. This property allows the compound to be effectively administered via the oral route in animal models to achieve sufficient systemic exposure for pharmacological activity. The compound likely exhibits favorable absorption and distribution characteristics typical of small molecule PDE4 inhibitors.
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| Toxicity/Toxicokinetics |
Specific toxicity data for WAY127093B racemate are not provided in the available sources. As a research compound for preclinical use, its safety profile has likely been evaluated in standard toxicological studies, including acute and sub-chronic toxicity assessments in rodents. The compound is intended for research use only and not for human therapeutic applications. Standard safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment.
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| References | |
| Additional Infomation |
WAY127093B racemate is a racemic mixture of WAY127093B. It is categorized as a phosphodiesterase IV inhibitor and is used in research related to inflammatory diseases. The compound's chemical structure is C23H28N4O4 with a molecular weight of 424.49. It is available in various pack sizes for research purposes and is typically stored as a powder at -20°C for long-term stability. This product is for research use only, not for human use.
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| Molecular Formula |
C23H28N4O4
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| Molecular Weight |
424.492825508118
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| Exact Mass |
424.211
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| CAS # |
145743-63-1
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| PubChem CID |
19792796
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
31
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| Complexity |
627
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C(CC(=O)N1C(=O)NCC2=CN=CC=C2)C3=CC(=C(C=C3)OC)OC4CCCC4
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| InChi Key |
JBTJXXDPSJKBRV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H28N4O4/c1-26-19(13-22(28)27(26)23(29)25-15-16-6-5-11-24-14-16)17-9-10-20(30-2)21(12-17)31-18-7-3-4-8-18/h5-6,9-12,14,18-19H,3-4,7-8,13,15H2,1-2H3,(H,25,29)
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| Chemical Name |
3-(3-cyclopentyloxy-4-methoxyphenyl)-2-methyl-5-oxo-N-(pyridin-3-ylmethyl)pyrazolidine-1-carboxamide
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| Synonyms |
WAY127093B racemate; WAY 127093B; WAY127093 B; WAY-127093B ;WAY-127093-B; WAY127093B; WAY 127093-B; WAY-127093B
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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 | 2.3558 mL | 11.7788 mL | 23.5577 mL | |
| 5 mM | 0.4712 mL | 2.3558 mL | 4.7115 mL | |
| 10 mM | 0.2356 mL | 1.1779 mL | 2.3558 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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