LASSBio-1135, also known as CHEMBL466188, is a synthetic antagonist of TRPV1 channels and a blocker of TNF-α channels. It has an effective concentration of 0.1-100 μM and an IC50 of 588 and 642 nM for TRPV1 and TNF-α receptors respectively. LASSbio belongs to a family of imidazo[1,2-a] pyridine derivatives and was found to be an inhibitor of p38 MAPK and COX2 in vivo. However, similar results have not been shown to this day in vitro where LASSbio failed to inhibit p38 MAPK directly and only slightly inhibited COX2. LASSbio is highly effective in completely reducing hyperalgesia induced by capsaicin and inhibits capsaicin evoked currents in a concentration dependent manner. LASSbio also inhibits TNF-α production in macrophages stimulated by LPS by reducing p38 MAPK activation through a modulation of an upstream signaling pathway thus making it a possible therapeutic agent for the prevention of neuropathic and other pain
产品描述
An Antagonist of TRPV1 Channels and TNF-alpha Receptors
