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Description: Selective TRPC3 inhibitor
Chemical Name: 1-[4-[(2,3,3-Trichloro-1-oxo-2-propen-1-yl)amino]phenyl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid
Purity: ≥98% (HPLC)
Biological Activity for Pyr3
Pyr3 is a selective antagonist of the canonical transient receptor potential channel 3 (TRPC3). Inhibits TRPC3-mediated Ca2+ influx (IC50 = 0.7 μM) and suppresses activation of nuclear factor of activated T cells (NFAT). Inhibits hypertrophic responses in cardiomyocytes.
Technical Data for Pyr3
| M. Wt | 456.63 |
| Formula | C16H11Cl3F3N3O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1160514-60-2 |
| PubChem ID | 56964346 |
| InChI Key | RZHGONNSASQOAY-UHFFFAOYSA-N |
| Smiles | O=C(/C(Cl)=C(Cl)\Cl)NC(C=C2)=CC=C2N1N=CC(C(OCC)=O)=C1C(F)(F)F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Pyr3
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.66 | 100 |
Preparing Stock Solutions for Pyr3
The following data is based on the product molecular weight 456.63. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.19 mL | 10.95 mL | 21.9 mL |
| 5 mM | 0.44 mL | 2.19 mL | 4.38 mL |
| 10 mM | 0.22 mL | 1.09 mL | 2.19 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets for Pyr3
References for Pyr3
References are publications that support the biological activity of the product.
Kiyonaka et al (2009) Selective and direct inhibition of TRPC3 channels underlies biological activities of a pyrazole compound. Proc.Natl.Acad.Sci. 106 5400
If you know of a relevant reference for Pyr3, please let us know.
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Keywords: Pyr3, Pyr3 supplier, canonical, transient, receptor, potential, TRPC3, channels, inhibitors, inhibits, TRPC, 3751, Tocris Bioscience
5 Citations for Pyr3
Citations are publications that use Tocris products. Selected citations for Pyr3 include:
Lee et al (2013) TRPM2 channels are required for NMDA-induced burst firing and contribute to H(2)O(2)-dependent modulation in substantia nigra pars reticulata GABAergic neurons. J Neurosci 33 1157 PMID: 23325252
Zhou et al (2014) Cerebellar modules operate at different frequencies. Elife 3 e02536 PMID: 24843004
Y S et al (2020) Hydrogen sulfide, oxygen, and calcium regulation in developing human airway smooth muscle. FASEB J 34 12991-13004 PMID: 32777143
Szteyn et al (2015) Divergence in endothelin-1- and bradykinin-activated store-operated calcium entry in afferent sensory neurons. Am J Physiol Regul Integr Comp Physiol 7 PMID: 25873305
Senadheera et al (2013) Enhanced contractility in pregnancy is associated with augmented TRPC3, L-type, and T-type voltage-dependent calcium channel function in rat uterine radial artery. ACS Chem Neurosci 305 R917 PMID: 23948776
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Reviews for Pyr3
Average Rating: 5 (Based on 1 Review.)
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Pyr3, a selective TRPC3 channel blocker in mesangial cell.
By
Hitesh Soni on 01/04/2018
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Mesangial Cell
For in vitro study to block the TRP ion channel and elucidate the mechanism of proliferation of mesangial cells under normal and high glucose conditions and to understand the role of TRP ion channels in diabetic nephropathy.
