General description
A cell-permeable pyrazole derivative that acts as a selective blocker of the transient receptor potential cation channel TRPC3-medated ROCE (receptor-operated Ca2+ entry) and inhibits Carbachol- (Cat. No. 212385) induced Ca2+ entry in TRPC3-expressing HEK293 cells (IC50 = 0.72 µM; by Fura-2), while exhibiting much reduced potency against Stim1 and Orai1-coupled CRAC (Ca2+ release-activated Ca2+) channel-mediated SOCE (store-operated Ca2+ entry) in RBL-2H3 cells (IC50 = 13.08 µM; by Fura-2). A great complement to Pyr2 (Cat. No. 203890), Pyr 3 (Cat. No. 648490), and Pyr6 (Cat. No. 203891) in Ca2+ signaling studies.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
TRPC3
Reversible: yes
Packaging
Packaged under inert gas
Preparation Note
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
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥98% (HPLC) |
| Quality Segment | 100 |
| form | semisolid,solid |
| potency | 720 nM IC50 |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | orange-brown, white to off-white |
| solubility | DMSO: 100 mg/mL |
| shipped in | wet ice |
| storage temp. | 2-8°C |
| SMILES string | FC(F)(F)c1[n](nc(c1)C(F)(F)F)c2ccc(cc2)N[S](=O)(=O)c3ccc(cc3)C |
| InChI | 1S/C18H13F6N3O2S/c1-11-2-8-14(9-3-11)30(28,29)26-12-4-6-13(7-5-12)27-16(18(22,23)24)10-15(25-27)17(19,20)21/h2-10,26H,1H3 |
| InChI key | CVALMMCIOLXHDM-UHFFFAOYSA-N |
