| Description | YM-58483 (BTP2) is a specific and effective inhibitor of CRAC channels and subsequent Ca2+ signals. |
| In vitro | 在多种过敏性哮喘模型,如气道高反应、早期和晚期支气管狭窄、抗原诱导的气道嗜酸性粒细胞中,YM-58483均有抑制效果,在大鼠和豚鼠器官中还出现白三烯、IL-4水平的降低.在GVHD小鼠中,YM-58483还可抑制抗宿主CTL反应、供体T细胞扩张及IFN-γ的产生.YM-58483（30 mg/kg,p.o.）对小鼠的一般活动没有明显影响[1]. |
| In vivo | 作为选择性SOCE阻滞剂,YM-58483在Jurkat T细胞中抑制anti-CD3抗体所诱导的持续性钙离子流入。它抑制CRAC、TRPC3和TRPC5通道、促进TRPM4通道,抑制细胞因子的产生（IL-2, IL-4, IL-5, IFN-γ等）及T细胞的增殖。通过抑制NF-AT的激活,YM-58483可抑制MLR相关的脾细胞增殖[1]。YM-58483对IL-2的产生和NF-AT驱动的启动子活性也有明显的抑制作用,但不影响Jurkat细胞中AP-1驱动的启动子活性[2]。 |
| Cell experiments | Jurkat cells (1×107 cells/ml) were tested with varying concentration of compounds for 30 min at 37°C. The cells were stimulated with 1 μM ionomycin for 30 min at 37°C. After stimulation, the cells were centrifuged at 200×g for 2 min, and were solubilized in 100 μl of Triton X-100 lysis buffer. The cell lysate was centrifuged at 15,000×g for 20 min; the clarified lysate was subjected to SDS-PAGE; and NF-ATc2 was detected by Western blotting with anti-NF-ATc2 mAb. (Only for Reference) |
| Synonyms | YM 58483, BTP2 |
| molecular weight | 421.32 |
| Molecular formula | C15H9F6N5OS |
| CAS | 223499-30-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 78 mg/mL (185.1 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 78 mg/mL (185.1 mM) |
| References | 1. Ohga K, et al. Int Immunopharmacol. 2008, 8(13-14):1787-92. 2. Ishikawa J, et al. J Immunol. 2003, 170(9):4441-9. |