Doxofylline

SKU: orb1224198

Description

Doxofylline is a phosphodiesterase inhibitor and a xanthine derivative drug for asthma.(In Vitro):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.Doxofylline (5, 10 μM; 48 h) suppresses LPS-induced expression of NADPH oxidase subunits and TXNIP 16HBE cells.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.Doxofylline (0.1-10 μM; 15 min) significantly reduces fMLP-induced leukocyte migration in BM cells (fMLP: Formyl-Methionyl-Leucyl-Phenylalanine).(In Vivo):Doxofylline (0.3, 1 mg/kg; i.p.; single) inhibits LPS-induced inflammation in the lungs of mice.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.

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Key Properties

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CAS Number	69975-86-6
MW	266.26
Purity	>98% (HPLC)
Formula	C₁₁H₁₄N₄O₄
SMILES	O=C(N1C)N(C)C2=C(N(CC3OCCO3)C=N2)C1=O
Target	PDE
Solubility	Ethanol: 2 mg/mL (7.51 mM); Water: 24 mg/mL (90.14 mM); DMSO: 53 mg/mL (199.06 mM)

Bioactivity

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In Vivo

Doxofylline (0.3, 1 mg/kg; i.p.; single) inhibits LPS-induced inflammation in the lungs of mice. 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. Animal model: Male BALB/c mice (6 to 8-week-old). Dosage: 0.3, 1 mg/kg. Administration: Intraperitoneal injection; single. Result: Significantly 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 reduced the number of circulating leukocytes in comparison to LPS-treated mice. Significantly reduced accumulation of neutrophils in the peribronchial area. Animal model: Male BALB/c mice (6 to 8-week-old). Dosage: 0.3 mg/kg. Administration: Intraperitoneal injection; pre-treat; single. Result: Significantly reduced the adhesion of cells to the vascular tissue, but not the rolling of cells along the vessel wall in mice. Significantly reduced the expression of ICAM-1 induced by LPS.

In Vitro

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. Doxofylline (5, 10 μM; 48 h) suppresses LPS-induced expression of NADPH oxidase subunits and TXNIP 16HBE cells. 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. Doxofylline (0.1-10 μM; 15 min) significantly reduces fMLP-induced leukocyte migration in BM cells (fMLP: Formyl-Methionyl-Leucyl-Phenylalanine). Cell Viability Assay Cell line: 16HBE cells. Concentration: 5, 10 μM. Incubation time: 48 h. Result: 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 Cell line: BM cells (from naive mice). Concentration: 0.1-10 μM Incubation time: 15 min (pretreat). Result: Notably surpressed positive migration of BM cells in response to fMLP.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Doxofylline | Ansimar | ABC-12-3 | ABC-1213 | ABC 1213 | ALT 07 | DO 309

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Doxofylline (orb1224198)

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Purity:	>99.99% (May vary between batches)
CAS Number:	69975-86-6
MW:	266.25
Formula:	C₁₁H₁₄N₄O₄

CAS Number:	1346599-13-0
MW:	270.28
Formula:	C₁₁H₁₀D₄N₄O₄

MW:	266.25
Formula:	C₁₁H₁₄D₀N₄O₄

CAS Number:	69975-86-6
MW:	266.25
Formula:	C₁₁H₁₄N₄O₄

Doxofylline

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Doxofylline (orb1224198)

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