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Roflumilast N-Oxide
（CAS RN：292135-78-5 Produkt-Nr.：R0217）
Struktur
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| Synonym | 3,5-Dichloro-4-[3-(cyclopropylmethoxy)-4-(difluoromethoxy)benzamido]pyridine 1-Oxide |
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Spezifikation
| Purity(HPLC) | min. 98.0 area% |
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| Elemental analysis(Nitrogen) | 6.00 to 7.00 % |
| Melting point | 179.0 to 183.0 deg-C |
Referenzen
| Reaxys-RN | 10715186 |
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GHS
| Piktogramm |
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| Signalwort | Achtung |
| Gefährliche und schädliche Eigenschaften |
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| Hinweis |
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Transportinformation
| HS-Nummer | 2933399990 |
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Antrag
Roflumilast N-Oxide: An Active Metabolite of Roflumilast, a Selective Phosphodiesterase 4 (PDE4) Inhibitor
Roflumilast N-oxide is an active metabolite of roflumilast [R0193] which is a selective phosphodiesterase 4 (PDE4) inhibitor. PDE4 is a key enzyme in the degradation of cyclic adenosine monophosphate (cyclic AMP) [A2381] and is centrally involved in the cytokine production of inflammatory cells. The inhibition of PDE4 activity leads to accumulation of intracellular cyclic AMP. Roflumilast N-oxide is also used for the treatment of chronic obstructive pulmonary disease (COPD). While the precise mechanism of the therapeutic action in COPD is not well defined, it is thought to be related to the effects of increased intracellular cyclic AMP in lung cells. (The product is for research purpose only.)
References
- Roflumilast inhibits leukocyte-endothelial cell interactions, expression of adhesion molecules and microvascular permeability
- Roflumilast N-oxide, a PDE4 inhibitor, improves cilia motility and ciliated human bronchial epithelial cells compromised by cigarette smoke in vitro
- Selective PDE inhibitors as novel treatments for respiratory diseases (a review)
- Sensitive quantification of roflumilast and roflumilast N-oxide in human plasma by LC-MS/MS employing parallel chromatography and electrospray ionisation
- Simultaneous quantitation of IC87114, roflumilast and its active metabolite roflumilast N-oxide in plasma by LC-MS/MS: application for a pharmacokinetic study
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