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PSB-06126 is an inhibitor of nucleoside triphosphate diphosphorylase 3 (NTPDase 3; IC50 = 1.5 µM for the rat enzyme).1 It is selective for NTPDase 3 over NTPDase 1 and -2 at 1 mM. PSB-06126 also activates large-conductance calcium-activated potassium channels (KCa/BK) in rabbit bladder smooth muscle preparations in an inside/out patch-clamp assay (EC50 = 0.841 µM) and inhibits UTP-induced calcium mobilization in 1321N1 astrocytoma cells expressing the human purinergic P2Y4 receptor (IC50 = 7.72 µM).2,3 It selectively increases extracellular ATP levels in isolated bone marrow-derived mesenchymal stem cells (BM-MSCs) isolated from postmenopausal women over those from young women when used at a concentration of 3 µM.4 PSB-06126 increases matrix mineralization in primary postmenopausal women BM-MSCs.
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1. Structure-
2. Development of GoSlo-
3. Development of potent and selective antagonists for the UTP-
4. Silencing NTPDase3 activity rehabilitates the osteogenic commitment of post-