2,5-dimethylcelecoxib, also known as DMC, is a synthetic opener of KV7 channels in smooth muscle cells. It is a derivative of Celecoxib without its COX-2 inhibitory function. In Asthma and other lung diseases, airways become hyperconstricted because of the secretion of various endogenous substances. DMC causes an increase in KV7 currents and restores current amplitudes in guinea pig ASMC (air smooth muscle cells). This effect is also seen after the application of bronchoconstrictors such as Methacholine and Histamine suggesting DMC can regulate and dilate airway diameter in bronchoconstricting diseases. DMC is a potent activator of apoptotic pathways and also suppresses production of prostaglandins in vitro by inhibiting cytokine-triggered upregulation of microsomal PGE-synthase-1. These properties may be valuable in the research of cancer.
产品描述
A KV7 Channel Opener
产品形式
KV7 or KCNQs are voltage-gated potassium channels. These channels are mainly responsible for the cardiac and auditory IKs current and the neuronal M-current but can be found in other tissues as well. Voltage-gated potassium channels are tetramers of α-subunits, which surround a K -selective pore. The different five Kv7 subtypes have distinct assembly preferences encoded by a C-terminal cytoplasmic assembly domain, the A-domain Tail. This domain is a self-assembling, parallel, four-stranded coiled coil.