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203891

Sigma-Aldrich

CRAC Channel Inhibitor III, Pyr6 - Calbiochem

Synonym(s):
CRAC Channel Inhibitor III, Pyr6 - Calbiochem, N-(4-(3,5-bis(trifluoromethyl)-1H-pyrazol-1-yl)phenyl)-3-fluoroisonicotinamide
Empirical Formula (Hill Notation):
C17H9F7N4O
Molecular Weight:
418.27

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.

Packaging

10 mg in Glass bottle
Packaged under inert gas

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Orai3

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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