General description
A cell-permeable pyrazole that acts as a more potent blocker of Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 590 nM by Fura-2; peak current density pA/pF = -1.13 and -7.50, respectively, with or without 3 µM BTP2/Pyr2 by whole cell clamp) than the transient receptor potential cation channel TRPC3-mediated ROCE (receptor-operated Ca2+ entry) inTRPC3-expressing HEK293 cells (IC50 = 4.21 µM by Fura-2; pA/pF = -1.54 and -18.50, respectively, with or without 3 µM BTP2/Pyr2). A great complement to Pyr 3 (Cat. No. 648490), Pyr6, and Pyr10 in Ca2+ signaling studies.
A cell-permeable pyrazole that acts as a more potent blocker of Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 590 nM by Fura-2; peak current density pA/pF = -1.13 and -7.50, respectively, with or without 3 µM BTP2/Pyr2 by whole cell clamp) than the transient receptor potential cation channel TRPC3-mediated ROCE (receptor-operated Ca2+ entry) inTRPC3-expressing HEK293 cells (IC50 = 4.21 µM by Fura-2; pA/pF = -1.54 and -18.50, respectively, with or without 3 µM BTP2/Pyr2). A great complement to Pyr 3 (Cat. No. 648490), Pyr6, and Pyr10 in Ca2+ signaling studies.
Biochem/physiol Actions
Primary Target
CRAC Channel
Target IC50: 590 nM by Fura-2
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Schleifier, H., et al. 2012. Br J PharmacolIn Press
Yonetoku, Y., et al. 2006. Bioorg. Med. Chem.14, 5370.
Yonetoku, Y., et al. 2006. Bioorg. Med. Chem.14, 4750.
Zitt, C., et al. 2004. J. Biol. Chem.279, 12927.
Trevillyan, J.M., et al. 2001. J. Biol. Chem.276, 48118.
Djuric, S.W., et al. 2000. J. Med. Chem.43, 2975.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
- UPC:
- 51311808
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 203890-5MG
- CAS:
- 223499-30-7