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Dooku1 is an antagonist of yoda1-activated Piezo1 ion channels (IC50 = 1.3 µM in HEK293 cells expressing the human receptor).1 It is selective for Piezo1 activated by yoda1 (Item No. 21904) over constituitively active Piezo1, transient receptor potential vanilloid 4 (TRPV4), and transient receptor potential canonical 4 (TRPC4) at 10 µM. Dooku1 (10 µM) reduces the percentage of cells with yoda1-induced extracellular phosphatidylserine exposure in red blood cells (RBCs) isolated from patients with sickle cell anemia.2 Preincubation with dooku1 (10 µM) inhibits yoda1-induced relaxation of isolated mouse aortic rings.1
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1. Yoda1 analogue (Dooku1) which antagonizes Yoda1-
2. Yoda1 and phosphatidylserine exposure in red cells from patients with sickle cell anaemia. Sci. Rep. 10(1), 20110 (2020).