Roflumilast N-oxide

  CAY-33975-10 10 mg

Data Sheet:     SDS:    

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292135-78-5  

A solid  

≥98%  

419,2  

-20  

-20  

1460  

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Description

 

Roflumilast N-oxide is an inhibitor of phosphodiesterase 4 (PDE4; IC50 = 2 nM) and an active metabolite of the PDE4 inhibitor roflumilast (Item No. 15141).{49692} It is selective for PDE4 over PDE1-3 and PDE5 (IC50s = >10,000 nM for all). It reduces TNF-α-induced ICAM-1 and eotaxin levels when used in combination with prostaglandin E2 (PGE2; Item No. 14010) in GM06114 human fetal lung fibroblasts (IC50s = 0.9 and 0.5 nM, respectively).{61405} It also reduces bFGF-induced and IL-1β augmented proliferation in the same cells. Roflumilast N-oxide (2 nM) reverses cigarette smoke extract-induced reductions in ciliary beat frequency in isolated human bronchial epithelial cells.{61406} Roflumilast N-oxide also increases plasma glucagon-like peptide 1 (GLP-1) levels in a glucose challenge in diabetic db/db mice when administered at a dose of 10 mg/kg, as well as prevents increases in blood glucose in db/db mice at 3 mg/kg per day.{61407}

 

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