TRPC3 Channel Inhibitor, Pyr3

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 µM 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 µM 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 Ca^{2+ signaling studies.}

Packaged under inert gas

Toxicity: Standard Handling (A)

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Schleifier, H., et al. 2012. Br J PharmacolIn Press
Kiyonaka, S., et al. 2009. Proc. Natl. Acad. Sci. USA106, 5400.

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