| Bioactivity | Doxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIP inflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm[1][2][3]. | ||||||||||||
| Target | Adenosine A1 receptor, phosphodiesterase IV. | ||||||||||||
| Invitro | Doxofylline (5, 10 µM; 48 h) shows potent protection against LPS-induced epithelial inflammation by reducing PGE2, NO release, and decreasing mitochondrial ROS generation in 16HBE cells[1].Doxofylline (5, 10 µM; 48 h) suppresses LPS-induced expression of NADPH oxidase subunits and TXNIP 16HBE cells[1].Doxofylline (5, 10 µM; 48 h) inhibits LPS-induced NLRP3 inflammasome activation and secretion of IL-1b and IL-18, as well as mitigates LPS-mediated SIRT1 reduction[1].Doxofylline (0.1-10 µM; 15 min) significantly reduces fMLP-induced leukocyte migration in BM cells (fMLP: Formyl-Methionyl-Leucyl-Phenylalanine)[2]. Cell Viability Assay[1] Cell Line: | ||||||||||||
| In Vivo | Doxofylline (0.3, 1 mg/kg; i.p.; single) inhibits LPS-induced inflammation in the lungs of mice[2].Doxofylline (0.3 mg/kg; i.p.; pre-treat; single) notably reduces the adhesion of cells to the vascular tissue and surpresses the expression of LPS-induced ICAM-1 in vivo[2]. Animal Model: | ||||||||||||
| Name | Doxofylline | ||||||||||||
| CAS | 69975-86-6 | ||||||||||||
| Formula | C11H14N4O4 | ||||||||||||
| Molar Mass | 266.25 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Doxofylline
CAS: 69975-86-6 F: C11H14N4O4 W: 266.25
Doxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cel
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