1315323-00-2

Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1].

Pyr10 is a novelselective inhibitor of the transient receptor potential channel TRPC3. Pyr10 blocks carbachol-induced calcium entry into TRPC3-transfected HEK293 cells (IC50 = 0.72 μM)with significantly lower activity against STIM1/Orai1 mediated release of calcium from endoplasmic reticulum (store operated calcium entry) in BRL-2H3 cells (IC50 = 13.08 μM).

TRPC3: 0.72 μM (IC₅₀)

Store at -20°C

[1] Schleifer H, et al. Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathways. Br J Pharmacol. 2012 Dec;167(8):1712-1722. DOI:10.1111/j.1476-5381.2012.02126.x
[2] Saliba Y, et al. Transient Receptor Potential Canonical 3 and Nuclear Factor of Activated T Cells C3 Signaling Pathway Critically Regulates Myocardial Fibrosis. Antioxid Redox Signal. 2019 Jun 1;30(16):1851-1879. DOI:10.1089/ars.2018.7545