Pyr10 是吡唑衍生物，是TRPC3通道的选择性抑制剂。Pyr10抑制卡巴可刺激的TRPC3转染的 HEK293 细胞中的 Ca2+流入。它具有区分受体操纵的TRPC3和天然基质相互作用分子 1 (STIM1)/Orai1 通道的能力。

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

The novel pyrazole Pyr10 displayed substantial selectivity for TRPC3-mediated responses (18-fold) and the selective block of TRPC3 channels by Pyr10 barely affected mast cell activation[1].

Pyr10 blunted ventricular CF activation and MF in l-NAME hypertensive mice.?Finally, TRPC3 was present in human ventricular CFs and upregulated in MF, whereas pharmacological modulation of TRPC3-NFATc3 decreased proliferation and collagen secretion.?TRPC3-NFATc3 signaling is modulated by P.E. and critically regulates ventricular CF phenotype and MF.?These findings strongly argue for P.E., through TRPC3 targeting, as potential and interesting therapeutics for MF management[2].

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C18H13F6N3O2S

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DMSO:95 mg/mL (211.4 mM),Need ultrasonic
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In solvent: -80°C for 2 years