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Drug intelligence / Profile preview
pyrazole 3
- Development stage
- Preclinical
- Modality
- Small Molecules
- Administration
- Intraperitoneal
01
Overview
Pyrazole 3 (Pyr3) is a selective, cell-permeable small molecule inhibitor of the transient receptor potential canonical 3 (TRPC3) channel. Originally identified by researchers at Kyoto University, Pyrazole 3 directly inhibits TRPC3-mediated calcium influx with an IC50 of approximately 0.7 μM. It also exhibits off-target inhibitory activity against STIM1/Orai1-mediated store-operated calcium entry (SOCE) at similar concentrations. Pyrazole 3 is widely utilized as a research tool to investigate TRPC3-mediated calcium signaling, cardiac hypertrophy, atrial fibrillation, and tissue fibrosis. However, its in vivo utility is limited by low metabolic stability, due to rapid ester hydrolysis to its inactive acid derivative, and potential toxicity from its reactive trichloroacrylic amide group.
- Other names
- CRAC Channel Inhibitor IIEthyl 1-{4-[(2,3,3-trichloroacryloyl)amino]phenyl}-5-(trifluoromethyl)-1H-pyrazole-4-carboxylatepyrazole-3pyrazole3pyrazole 3
02
Targets
TRPC3
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