TRPC3 Channel Inhibitor III, Pyr10

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 µM; 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 µM; 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 µM; by Fura-2; peak current density pA/pF = -1.01 and -18.50, respectively, with or without 3 µM 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 µM; by Fura-2; pA/pF = -4.39 and -7.50, respectively, with or without 3 µM Pyr10). A great complement to Pyr2 (Cat. No. 203890), Pyr 3 (Cat. No. 648490), and Pyr6 (Cat. No. 203891) in Ca²⁺ signaling studies.

Cell permeable: yes

Primary Target
TRPC3

Reversible: yes

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.

Schleifer, H. et al. 2012. Br. J. Pharmacol.167, 1712.

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