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Beschreibung

A cell-permeable pyrazole derivative that acts as a selective blocker of the transient receptor potential cation channel TRPC3-medated ROCE (receptor-operated Ca2+ entry) and inhibits Carbachol- (Cat. No. 212385) induced Ca2+ entry in TRPC3-expressing HEK293 cells (IC50 = 0.72 µ,M, by Fura-2), while exhibiting much reduced potency against Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 13.08 µ,M, by Fura-2). A great complement to Pyr2 (Cat. No. 203890), Pyr 3 (Cat. No. 648490), and Pyr6 (Cat. No. 203891) in Ca2+ signaling studies., A cell-permeable pyrazole derivative that acts as a selective blocker of the transient receptor potential cation channel TRPC3-medated ROCE (receptor-operated Ca2+ entry) and inhibits Carbachol- (Cat. No. 212385) induced Ca2+ entry in TRPC3-expressing HEK293 cells (IC50 = 0.72 µ,M, by Fura-2, peak current density pA/pF = -1.01 and -18.50, respectively, with or without 3 µ,M Pyr10 by whole cell clamp), while exhibiting much reduced potency against Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 13.08 µ,M, by Fura-2, pA/pF = -4.39 and -7.50, respectively, with or without 3 µ,M Pyr10). A great complement to Pyr2 (Cat. No. 203890), Pyr 3 (Cat. No. 648490), and Pyr6 (Cat. No. 203891) in Ca2+ signaling studies.