trans-Ned 19

trans-Ned 19 is a NAADP antagonist and TPC blocker. trans-Ned 19 suppresses the calcium signal and the rat aorta relaxation in response to low histamine concentrations. trans-Ned 19 increases the spontaneous acrosome reaction rate, alleviates anti-CD3 mAb-induced intestinal inflammation, and improves kidney damage in mice with nephrotoxic serum nephritis^{[1][2][3][4][5][6]}. IC50 & Target:NAADP, TPC, Calcium Channel^[1] In Vitro: trans-Ned 19 (25-100 μM; 1 h) inhibits T cell receptor (TCR)-stimulated Ca²⁺ signaling, cell activation and proliferation in primary naive CD4⁺ T cells from C57BL/6N mice^[1].
trans-Ned 19 (25-50 µM; 10 min) inhibits Norepinephrine (HY-13715)-induced Ca²⁺ elevation in rat aortic smooth muscle cells in a concentration-dependent manner^[2].
trans-Ned 19 (10 µM) causes lysosomal cholesterol accumulation in human umbilical vein endothelial cells, inhibits CD63 transport from late endosomes/lysosomes to Weibel-Palade bodies, and reduces the amount of CD63 associated with Weibel-Palade bodies^[3].
trans-Ned 19 (100 μM; 30 min) significantly increases the spontaneous acrosome reaction rate in acrosome reaction assay performed on permeabilized mouse sperm^[5].
In Vivo: trans-Ned 19 (20 mg/kg; i.p.; once administered 2 h before the first injection of anti-CD3 mAb and again 48 h later) reduces disease severity in a mouse model of intestinal inflammation induced by anti-CD3 mAb, as reflected by reduced weight loss^[1].
trans-Ned 19 (20 mg/kg; i.p.; once administered 2 h before the first injection of anti-CD3 antibody and then once daily for 3 days or once administered 2 h before the injection of nephrotoxic serum and then once daily for 10 days) improves disease progression and reduces weight loss in a mouse model of transient intestinal inflammation induced by CD3-specific antibody, and improves renal damage in mice with nephrotoxic serum nephritis^[4].