Doxofylline; Ansimar; ABC-1213; ALT-07; DO-309; Diprophylline; Lufyllin; Corphyllin; Neothylline;ABC 1213; ALT 07; DO 309; ABC1213; ALT07; DO309
| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| Other Sizes |
|
Doxofylline (also known as Neothylline; Ansimar; ABC-1213; ALT-07; Lufyllin; DO-309; Diprophylline; Corphyllin; ABC-12-3), a xanthine derivative, is a novel and potent PDE (phosphodiesterase) inhibitor with the potential for treating asthma. Doxofylline's mechanism of action is related to the inhibition of phosphodiesterase activities, but it appears to have decreased affinities towards adenosine A1 and A2 receptors, which may account for its better safety profile.
| ln Vitro |
Doxofylline (5, 10 µM; 48 h) reduces PGE2, NO release, and mitochondrial ROS generation in 16HBE cells, demonstrating strong protection against LPS-induced epithelial inflammation[1]. LPS-induced expression of NADPH oxidase subunits and TXNIP 16HBE cells is suppressed by doxofylline (5, 10 µM; 48 h)[1]. Doxofylline (5, 10 µM; 48 h) attenuates LPS-mediated SIRT1 reduction and prevents LPS-induced NLRP3 inflammasome activation and IL-1b and IL-18 secretion[1]. In BM cells, doxofylline (0.1–10 µM; 15 min) dramatically inhibits leukocyte migration induced by fMLP (formyl–methionyl–leucyl–phenylalanine)[2].
|
|---|---|
| ln Vivo |
In mice, doxofylline (0.3, 1 mg/kg; ip; single) reduces inflammation brought on by LPS in the lungs[2]. Doxofylline (0.3 mg/kg; ip; pre-treat; single) suppresses the production of LPS-induced ICAM-1 in vivo and dramatically decreases cell adherence to vascular tissue[2].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: 16HBE cells Tested Concentrations: 5, 10 µM Incubation Duration: 48 h Experimental Results: Weakened LPS-induced NO and PGE2 in a dose-dependent manner. Exerted dose-dependent inhibition on LPS-induced mitochondrial ROS production and NADPH oxidase subunits expression. Suppressed LPS- induced TXNIP expression and NLRP3 inflammasome activation at the protein level in a dose-dependent manner. Inhibited LPS-induced secretion of IL-1b and IL-18. Cell Viability Assay[2] Cell Types: BM cells (from naive mice) Tested Concentrations: 0.1-10 µM Incubation Duration: 15 min (pretreat) Experimental Results: Notably suppressed positive migration of BM cells in response to fMLP. |
| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse (6 to 8weeks old)[2].
Doses: 0.3, 1 mg/kg Route of Administration: intraperitoneal (ip)injection; single. Experimental Results: Dramatically inhibited the migration of neutrophils and the release of IL-6 and TNF-a into the lung lumen. Increased the bone marrow leukocyte numbers to levels similar to those seen in the saline-treated group. Notably decreased the number of circulating leukocytes in comparison to LPS-treated mice. Dramatically decreased accumulation of neutrophils in the peribronchial area. Animal/Disease Models: Male balb/c (Bagg ALBino) mouse (6 to 8weeks old)[2]. Doses: 0.3 mg/kg Route of Administration: intraperitoneal (ip)injection; pre-treat; single. Experimental Results: Dramatically decreased the adhesion of cells to the vascular tissue, but not the rolling of cells along the vessel wall in mice. Dramatically decreased the expression of ICAM-1 induced by LPS. |
| References |
[1]. Jiao P, et al. The protective effect of doxofylline against lipopolysaccharides (LPS)-induced activation of NLRP3 inflammasome is mediated by SIRT1 in human pulmonary bronchial epithelial cells. Artif Cells Nanomed Biotechnol. 2020 Dec;48(1):687-694.
[2]. Riffo-Vasquez Y, et al. Doxofylline, a novofylline inhibits lung inflammation induced by lipopolysacharide in the mouse. Pulm Pharmacol Ther. 2014 Apr;27(2):170-8. [3]. Shukla D, et al. Doxofylline: a promising methylxanthine derivative for the treatment of asthma and chronic obstructive pulmonary disease. Expert Opin Pharmacother. 2009 Oct;10(14):2343-56. |
| Molecular Formula |
C11H14N4O4
|
|
|---|---|---|
| Molecular Weight |
266.25
|
|
| CAS # |
69975-86-6
|
|
| Related CAS # |
Doxofylline-d6;1219805-99-8;Doxofylline-d4;1346599-13-0
|
|
| SMILES |
O1C([H])([H])C([H])([H])OC1([H])C([H])([H])N1C([H])=NC2=C1C(N(C([H])([H])[H])C(N2C([H])([H])[H])=O)=O
|
|
| Synonyms |
|
|
| 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) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7559 mL | 18.7793 mL | 37.5587 mL | |
| 5 mM | 0.7512 mL | 3.7559 mL | 7.5117 mL | |
| 10 mM | 0.3756 mL | 1.8779 mL | 3.7559 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
