Pyr3

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Cat.No. 3751 - Pyr3 | C16H11Cl3F3N3O3 | CAS No. 1160514-60-2
Description: Selective TRPC3 blocker
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)
Datasheet
Citations (4)
Reviews (1)
Literature (1)

Biological Activity

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

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

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.66 100

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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References

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


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Keywords: Pyr3, Pyr3 supplier, canonical, transient, receptor, potential, TRPC3, channels, inhibitors, inhibits, TRPC, 3751, Tocris Bioscience

4 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

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

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

Zhou et al (2014) Cerebellar modules operate at different frequencies. Elife 3 e02536 PMID: 24843004


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Reviews for Pyr3

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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.

PMID: 29273760 Reference
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Literature in this Area

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