Pyr6
Product Specifications
Product Name Alternative
N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide
UNSPSC Description
Pyr6 is a selective inhibitor of TRPC3 with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).
IC50 value: 0.49 uM [1]
Target: TRPC3 inhibitor
Pyr6 is a selective SOCE inhibitor (Yonetoku et al., 2008; Sweeney et al., 2009), Pyr6 displayed 37-fold (1.58 OM) higher potency for RBL SOCE than for TRPC3 ROCE, with an IC50 comparable to that of Pyr2 and Pyr3. Pyr6 at 3 uM diminished TRPC3 currents to only 52%. Consistent with inhibition of Orai channel activity Pyr2, Pyr3 or Pyr6 substantially inhibited typical Orai downstream signalling events in RBL mast cells (NFAT activation and degranulation) activated by passive store depletion.
Target Antigen
TRP Channel
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel;Neuronal Signaling
Field of Research
Others
Assay Protocol
https://www.medchemexpress.com/Pyr6.html
Purity
98.47
Solubility
DMSO : ≥ 100 mg/mL
Smiles
O=C(C1=C(F)C=NC=C1)NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2
Molecular Weight
418.27
References & Citations
[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):1712-22.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-12504/Pyr6-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-12504/Pyr6-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
245747-08-4
Available Sizes
Curated Selection
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