UniPR1331

UniPR1331 is an orally active 3β-hydroxy-Δ5-choline acid derivative that inhibits Eph-ephrin interactions. UniPR1331 blocks the interaction of VEGFR2 with its natural ligand vascular endothelial growth factor and inhibits subsequent autophosphorylation, signaling, and pro-angiogenic activation of endothelial cells. UniPR1331 exhibits anti-angiogenesis, anti-cancer and anti-inflammation effects. UniPR1331 can be used for the researches of cancer and inflammation, such as glioma and colitis^[1][2][3]. In Vitro:UniPR1331 (4-40 μM) specifically binds to human VEGFR2 (K_d = 62.2 μM) and EphA2 (K_d = 3.3 μM), and competes with VEGF for VEGFR2 binding (IC₅₀ = 16 μM) and ephrin-A1 for EphA2 binding (IC₅₀ = 4 μM)^[1].
UniPR1331 (10-30 μM, 10 mins) inhibits VEGF-induced VEGFR2 phosphorylation (IC₅₀ = 22 μM) in HUVECs^[1].
UniPR1331 (10-30 μM, 24-48 h) inhibits VEGF-induced proliferation, migration and endothelial sprout formation in HUVECs^[2].
UniPR1331 (3-30 μM, 24 h) maintains cells viability above 90% and inhibits TNFα release in mouse splenic lymphocytes treated with PMA (HY-18739) + Ionomycin (HY-13434)^[2].
UniPR1331 inhibits tube formation of human umbilical vein endothelial cells (HUVEC) (IC₅₀ = 2.9 μM) and human brain microvascular endothelial cells (HBMVEC) (IC₅₀ = 3.9 μM)^[3].
UniPR1331 (10 μM, 24 h) inhibits ephrin-A1-induced EphA2 phosphorylation in U87MG glioma cells and decreases EphA2 protein expression^[3].
In Vivo:UniPR1331 (50 μM, perivitelline space injection, 48 h post-fertilization) reduces the number and total length of ectopic vessel sprouts in the zebrafish yolk membrane angiogenesis model injected with U251 glioblastoma cells^[1].
UniPR1331 (10-25 mg/kg, p.o.) shows anti-inflammation effect in the TNBS-induced colitis model of C57BL/6 mice^[2].
UniPR1331 (30 mg/kg, p.o., 5 days a week for 30 days) inhibits tumor growth and prolongs survival in CD1-nu/nu mice with U87MG glioma subcutaneous and intracranial xenografts^[3].