VPC 51299
(R,E)-(3-palmitamido-4-(4-((4-(2,2,2-trifluoroethoxy)pyridin-2-yl)methoxy)phenyl)but-1-en-1-yl)phosphonic acid
VPC51299 is a potent low micromolar inhibitor containing a vinyl phosphonate head group and possessing a half-life of approximately 90 min in rats when dosed intravenously. Previously developed LPA1/LPA3 receptor antagonists contain a labile phosphate head group which impairs evaluation of scaffold LPA receptor antagonists in vivo. VPC51299 has replaced the phosphate with a more stable head group while retaining potency at both LPA1 and LPA3 to facilitate future in vivo studies of the biological functions of these receptors.Refer: J.E. East, et al. (2011). Development of a phosphatase-resistant, L-tyrosine derived LPA1/LPA3 dual antagonist. Medchemcomm 2:325-330.
This product is covered by Patent Number US 8,283,339 B2. Avanti manufactures this under license from University of Virginia.