For research use only. Not for therapeutic Use.
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1].
Pyr10 has the ability to discriminate between the classical Orai-mediated, highly Ca2+ selective signalling pathway and the phospholipase C-dependent Ca2+ entry-mediated by TRPC channels, specifically by TRPC3. Pyr10 (3 μM) completely eliminates TRPC3 currents as well as Ca2+ entry while exerting modest effects on Orai-mediated responses. The selective block of TRPC3 channels by Pyr10 barely affected mast cell activation[1].
Genetic deletion (TRPC3-/-) and pharmacological channel blockade with Pyr10 blunts ventricular cardiac fibroblast activation and myocardial fibrosis in N(ω)-nitro-l-arginine methyl ester (l-NAME) hypertensive mice[2].
| Catalog Number | I001211 |
| CAS Number | 1315323-00-2 |
| Synonyms | N-[4-[3,5-bis(trifluoromethyl)pyrazol-1-yl]phenyl]-4-methylbenzenesulfonamide |
| Molecular Formula | C18H13F6N3O2S |
| Purity | ≥95% |
| InChI | 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 |
| InChIKey | CVALMMCIOLXHDM-UHFFFAOYSA-N |
| SMILES | CC1=CC=C(C=C1)S(=O)(=O)NC2=CC=C(C=C2)N3C(=CC(=N3)C(F)(F)F)C(F)(F)F |
| Reference | [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):1712-1722. [2]. Saliba Y, et al. Transient Receptor Potential Canonical 3 and Nuclear Factor of Activated T Cells C3 Signaling Pathway Critically Regulates Myocardial Fibrosis. Antioxid Redox Signal. 2019 Jun 1;30(16):1851-1879. |
