| Name | Pyr10 |
| Description | Pyr10 is a pyrazole derivative and a selective TRP cation 3 inhibitor that distinguishes 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) and has an IC50 of 13.08 μM for store-operated Ca2+ entry in BRL-2H3 cells. |
| In vitro | 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]. |
| In vivo | 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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| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 95 mg/mL (211.41 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.34 mM), Sonication is recommended.
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| Keywords | TRPVChannel | TRPV Channel | TRPChannel | TRPC3 | TRP Channel | Transient receptor potential channels | STIM1 | SOCE | ROCE | pyrazole | Pyr-10 | Pyr10 | Pyr 10 | Orai | l-NAME | Inhibitor | inhibit | fibroblast | cardiac | Ca2+ |
| Inhibitors Related | (+)-Camphor | Rosiglitazone | Caffeic Acid | Oleoyl Serotonin | (-)-Menthol | Camphor | Probenecid | Pregnenolone | Nonivamide | 1,4-Cineole | trans-Cinnamaldehyde | Methyl salicylate |
| Related Compound Libraries | Pain-Related Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Ion Channel Targeted Library | Anti-Cancer Compound Library |
United States
