Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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) .
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
5 mg | In stock | $ 54.00 | |
10 mg | In stock | $ 89.00 | |
50 mg | In stock | $ 346.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 58.00 |
Description | 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) . |
Targets&IC50 | TRPC3:0.72 μM |
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]. |
Molecular Weight | 449.37 |
Formula | C18H13F6N3O2S |
CAS No. | 1315323-00-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 95 mg/mL (211.4 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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Pyr10 1315323-00-2 Membrane transporter/Ion channel TRP/TRPV Channel l-NAME pyrazole SOCE Inhibitor TRPC3 fibroblast cardiac ROCE inhibit Orai STIM1 Pyr 10 Transient receptor potential channels Ca2+ TRP Channel Pyr-10 inhibitor