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Pyr10

Catalog No. T16686   CAS 1315323-00-2

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) .

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Pyr10 Chemical Structure
Pyr10, CAS 1315323-00-2
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
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Purity: 99.7%
Purity: 99.46%
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Biological Description
Chemical Properties
Storage & Solubility Information
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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 95 mg/mL (211.4 mM), sonification is recommended.

TargetMolReferences and Literature

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. 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.

Related compound libraries

This product is contained In the following compound libraries:
Ion Channel Inhibitor Library Neuronal Signaling Compound Library Anti-Cancer Compound Library NO PAINS Compound Library Bioactive Compounds Library Max Bioactive Compound Library Inhibitor Library

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Keywords

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

 

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