| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
Arofylline targets phosphodiesterase 4 (PDE4) as a selective inhibitor. PDE4 is an enzyme responsible for the hydrolysis of cyclic AMP (cAMP) in immune cells. By inhibiting PDE4, Arofylline increases intracellular cAMP levels, leading to anti-inflammatory effects. The compound's selectivity for PDE4 over other phosphodiesterase isoforms contributes to its potential as an anti-inflammatory agent for asthma treatment.
|
|---|---|
| ln Vitro |
In vitro, Arofylline is a selective PDE4 inhibitor with anti-inflammatory effects. Its ability to inhibit PDE4 activity and increase cAMP levels has been characterized in various cell-based assays. The compound's anti-inflammatory effects have been demonstrated in immune cell models. Studies have examined its effects on cytokine production, immune cell activation, and inflammatory mediator release.
|
| ln Vivo |
In vivo, Arofylline has been studied as a potential treatment for asthma. Its anti-inflammatory effects support its potential as a therapeutic agent for respiratory inflammatory conditions. Studies have examined its effects in animal models of asthma and airway inflammation. Its pharmacokinetic properties and tolerability have been characterized in preclinical studies.
|
| Enzyme Assay |
In cell-free biochemical assays, Arofylline is evaluated for its inhibitory activity against PDE4. Enzyme activity assays measure the compound's ability to inhibit PDE4-mediated hydrolysis of cAMP. Its selectivity for PDE4 over other phosphodiesterase isoforms is assessed. Its purity and molecular weight (304.73 g/mol) are characterized using analytical techniques. These assays confirm the compound's mechanism as a selective PDE4 inhibitor.
|
| Cell Assay |
Cellular assays for Arofylline involve evaluating its effects on PDE4 activity and cAMP levels in immune cells. The compound's ability to increase intracellular cAMP and inhibit inflammatory responses is assessed. Its effects on cytokine production, immune cell activation, and inflammatory mediator release are studied in relevant cell models.
|
| Animal Protocol |
Animal models for Arofylline include models of asthma and airway inflammation. The compound is typically administered orally or via inhalation. Studies have examined its effects on airway hyperresponsiveness, inflammation, and lung function. Its pharmacokinetic properties have been characterized in preclinical species.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data for Arofylline show that the compound has a molecular weight of 304.73 g/mol with a molecular formula of C14H13ClN4O2. The CAS number is 136145-07-8. The compound has a density of 1.4±0.1 g/cm3 and a boiling point of 562.6±56.0 °C. Standard handling procedures for PDE4 inhibitor research compounds apply.
|
| Toxicity/Toxicokinetics |
The toxicity profile of Arofylline has not been extensively documented in publicly available sources. As a PDE4 inhibitor, standard safety precautions for handling pharmaceutical research compounds apply. The compound is for research use only and not for human use.
|
| Additional Infomation |
Arofylline is a selective PDE4 inhibitor with anti-inflammatory effects being investigated for asthma treatment. It has a molecular weight of 304.73 g/mol and formula C14H13ClN4O2. The CAS number is 136145-07-8.
|
| Molecular Formula |
C14H13CLN4O2
|
|---|---|
| Molecular Weight |
304.734
|
| Exact Mass |
304.073
|
| CAS # |
136145-07-8
|
| PubChem CID |
166553
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.429g/cm3
|
| Boiling Point |
562.6ºC at 760 mmHg
|
| Flash Point |
294ºC
|
| Vapour Pressure |
1.1E-12mmHg at 25°C
|
| Index of Refraction |
1.642
|
| LogP |
1.938
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
21
|
| Complexity |
425
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCCN1C(=O)C2N=CNC=2N(C2=CC=C(Cl)C=C2)C1=O
|
| InChi Key |
GVTLDPJNRVMCAL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H13ClN4O2/c1-2-7-18-13(20)11-12(17-8-16-11)19(14(18)21)10-5-3-9(15)4-6-10/h3-6,8H,2,7H2,1H3,(H,16,17)
|
| Chemical Name |
3-(4-chlorophenyl)-1-propyl-7H-purine-2,6-dione
|
| Synonyms |
Arofylline LAS 31025 Arofyllin
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 3.2816 mL | 16.4080 mL | 32.8159 mL | |
| 5 mM | 0.6563 mL | 3.2816 mL | 6.5632 mL | |
| 10 mM | 0.3282 mL | 1.6408 mL | 3.2816 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
