Customization: | Available |
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Powder: | Yes |
Customized: | Customized |
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Product name | Roflumilast |
Apperance | White Powder |
Cas number | 162401-32-3 |
MF | C17H14Cl2F2N2O3 |
MW | 403.2075 |
Rofistat selectively inhibits PDE4, blocks the transmission of inflammatory response signals, and thus inhibits the damage caused by respiratory diseases such as COPD and asthma to lung tissue: cyclic nucleotides cAMP and cGMP are important second messengers in cells, playing an important role in various biological reactions caused by extracellular signals including hormones, auto active substances, and neurotransmitters. Phosphodiesterase (PDE) is a key enzyme that hydrolyzes intracellular cAMP or cGMP into inactive single nucleotides, and is the only pathway for the hydrolysis of cAMP and cGMP. The PDE family has 11 different members, namely PDE1 to PDE11, which are expressed differently in different tissues and cells. They differ from each other in terms of structure, biochemistry, and pharmacological properties. PDE4 is the main regulator of cAMP metabolism, the main PDE isoform of inflammatory and immune cells, and also the main PDE isoform distributed in the lungs. It is the largest group in the PDE family, with four subtypes (PDE4A, B, C, D). Each subtype originates from a different gene and contains multiple variants. Various PDF4 molecules have three highly homologous regions: the hydrolysis catalytic site located from the center to the C-terminus, and two upstream conserved regions (UCR1 and UCR2). PDE4 is associated with cAMP hydrolysis in various inflammatory cells. Since cAMP can cause bronchial smooth muscle relaxation and pulmonary inflammatory response, inhibiting PDE4 can reduce the release of inflammatory mediators, thereby inhibiting the damage caused by respiratory diseases such as COPD and asthma to lung tissue.