203891
CRAC Channel Inhibitor III, Pyr6
Synonym(s):
CRAC Channel Inhibitor III, Pyr6, N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-3-fluoroisonicotinamide
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About This Item
Empirical Formula (Hill Notation):
C17H9F7N4O
Molecular Weight:
418.27
UNSPSC Code:
12352200
Recommended Products
assay
≥99% (HPLC)
Quality Level
form
solid
potency
490 nM IC50
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
light beige
solubility
DMSO: 100 mg/mL
shipped in
wet ice
storage temp.
2-8°C
General description
A cell-permeable pyrazole derivative that acts as a selective blocker of Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 490 nM by Fura-2), while exhibiting much reduced potency against the transient receptor potential cation channel TRPC3-medated ROCE (receptor-operated Ca2+ entry) upon carbachol (Cat. No. 212385) stimulation in TRPC3-expressing HEK293 cells (IC50 = 18.46 µM; by Fura-2). A great complement to Pyr2 (Cat. No. 203890), Pyr3 (Cat. No. 648490), and Pyr10 (Cat. No. 648494) in Ca2+ signaling studies.
A cell-permeable pyrazole derivative that acts as a selective blocker of Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 490 nM by Fura-2; peak current density pA/pF = -1.31 and -7.50, respectively, with or without 3 µM Pyr6 by whole cell clamp), while exhibiting much reduced potency against the transient receptor potential cation channel TRPC3-medated ROCE (receptor-operated Ca2+ entry) upon carbachol (Cat. No. 212385) stimulation in TRPC3-expressing HEK293 cells (IC50 = 18.46 µM; by Fura-2; pA/pF = -9.50 and -18.50, respectively, with or without 3 µM Pyr6). A great complement to Pyr2 (Cat. No. 203890), Pyr3 (Cat. No. 648490), and Pyr10 (Cat. No. 648494) in Ca2+ signaling studies.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Orai3
Orai3
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Schleifer, H., et al. 2012. Br. J. Pharmacol.167, 1712.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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