TPRC3 Channel Inhibitor III; Pyr10

Biochem/physiol Actions

Primary TargetTRPC3

Reversible: yes

Cell permeable: yes

General description

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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

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

Packaging

Packaged under inert gas

10 mg in Glass bottle

Reconstitution

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

Warning

Toxicity: Standard Handling (A)