compound introduction
UCB-5307 is a potent TNF signaling inhibitor with a K D of 9 nM for human TNFα. UCB-5307 can penetrate the preformed hTNF/hTNFR1 complex. In Vitro UCB-5307 inhibits wild-type TNF but does not inhibit L57F TNF. The T 1/2 of UCB-5307 is 3.3 h. UCB-5307 disrupts a preformed hTNF/hTNFR1 complex, can penetrate the preformed complex, dislodging one of the receptors. Preloading hTNF with UCB-5307 blocks one receptor from binding. UCB-5307 binds to a pocket in the centre of the TNF trimer formed by the movement of the TNF monomers, stabilising the distorted trimer, which leads to reduced signalling through TNFR1. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid
