Roflumilast

Description

What is Roflumilast?

Roflumilast is an orally available, long-acting inhibitor of phosphodiesterase (PDE) type 4 (PDE4), with anti-inflammatory and potential antineoplastic activities. Upon administration, roflumilast and its active metabolite roflumilast N-oxide selectively and competitively bind to and inhibit PDE4, which leads to an increase of both intracellular levels of cyclic-3′,5′-adenosine monophosphate (cAMP) and cAMP-mediated signaling. cAMP prevents phosphorylation of spleen tyrosine kinase (SYK) and abrogates activation of the PI3K/AKT/mTOR signaling pathway, which may result in the induction of apoptosis.

PDE4, a member of the PDE superfamily that hydrolyses cAMP and 3′,5′-cyclic guanosine monophosphate (cGMP) to their inactive 5′ monophosphates, is upregulated in a variety of cancers and may contribute to chemoresistance; it also plays a key role in inflammation, especially in inflammatory airway diseases.

Basic information

Product Name:	Roflumilast
Synonyms:	Daliresp; Roflumilast INN; roflumilastum
CAS:	162401-32-3
MF:	C17H14Cl2F2N2O3
MW:	403.21
EINECS:	685-382-2
Product Categories:	Pharmaceutical intermediate;Bulk Drug Intermediates;Asthma drugs;APIs;Respiratory Drugs

Chemical Structure

Roflumilast

Chemical Properties

Melting point	158°C
Boiling point	430.6±45.0 °C(Predicted)
density	1.471±0.06 g/cm3(Predicted)
storage temp.	-20°C
solubility	DMSO: soluble20mg/mL, clear
form	powder
pka	9.89±0.70(Predicted)
color	white to beige

Roflumilast Uses

Roflumilast is a benzamide obtained by formal condensation of the carboxy group of 3-(cyclopropylmethoxy)-4-(difluoromethoxy)benzoic acid with the amino group of 3,5-dichloropyridin-4-amine. Used for treatment of bronchial asthma and chronic obstructive pulmonary disease. It has a role as a phosphodiesterase IV inhibitor and an anti-asthmatic drug. It is a member of benzamides, a chloropyridine, an aromatic ether, an organofluorine compound and a member of cyclopropanes.

It is also a selective phosphodiesterase 4(PDE4) inhibitor in treatment of chronic obstructive pulmonary disease.

Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

MSDS: MSDS available.

COA: COA can be available if you send us inquiry.

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