Pyr10是一种新型TRPC3选择性抑制剂,作用于转染YFP-TRPC3的HEK293细胞,抑制ROCE,IC50为0.72uM。
| Cas No. | 1315323-00-2 |
| Canonical SMILES | O=S(C1=CC=C(C)C=C1)(NC2=CC=C(N3N=C(C(F)(F)F)C=C3C(F)(F)F)C=C2)=O |
| 分子式 | C18H13F6N3O2S |
| 分子量 | 449.37 |
| 溶解度 | DMSO : 100 mg/mL (222.53 mM);Water :< 0.1 mg/mL (insoluble) |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Pyr10is a novel TRPC3-selective inhibitor, IC50 of Ca2+ influx inhibition by Pyr10 in carbachol-stimulated YFP-TRPC3-transfected HEK293 cells for ROCE and thapsigargin-depleted native RBL-2H3 cells for SOCE is 0.72 uM and 13.08 uM.IC50 value: 0.72 uM (TRPC3-ROCE), 13.08 uM (SOCE) [1]Target: TRPC3in vitro: Pyr10 displays substantial selectivity for TRPC3-mediated responses (18-fold) and the selective block of TRPC3 channels by Pyr10 barely affected mast cell activation.[1] [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]. Obermayer D, et al. Microwave-assisted and continuous flow multistep synthesis of 4-(pyrazol-1-yl)carboxanilides. J Org Chem. 2011 Aug 19;76(16):6657-6669. |
