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Beschreibung

A cell-permeable pyrazole that acts as an equally potent blocker of Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 540 nM by Fura-2, peak current density pA/pF = -1.45 and -7.50, respectively, with or without 3 µ,M BTP2/Pyr3 by whole cell clamp) and the transient receptor potential cation channel TRPC3-mediated ROCE (receptor-operated Ca2+ entry) in TRPC3-expressing HEK293 cells (IC50 = 540 nM, by Fura-2, pA/pF = -2.27 and -18.50, respectively, with or without 3 µ,M BTP2/Pyr3). Pyr3 is also demonstrated to alleviate pressure overload-induced cardiac hypertrophy following TAC (transverse aortic constriction) operation in mice (0.1 mg/kg/day via i.p. osmotic pump) in vivo. A great complement to Pyr 2 (Cat. No. 203890), Pyr6, and Pyr10 in Ca2+ signaling studies.