| Description | PD151746 is a calpain inhibitor with a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM). Its IC50 values are 0.26 ± 0.03 μM (Ki for μ-calpain) and 5.33 ± 0.77 μM (Ki for m-calpain) [1]. In vitro, PD151746 targets calpain and reduces oxLDL-induced cytotoxicity [2]. |
| In vivo | PD151746可使HMEC-1细胞中氧化型低密度脂蛋白诱导的细胞毒性降低。PD151746有效减弱SY5Y细胞中鱼毒素诱导的SLLVY-AMC水解作用。 |
| Target activity | m-Calpain:5.33 μM, μ-Calpain:260 nM |
| molecular weight | 237.25 |
| Molecular formula | C11H8FNO2S |
| CAS | 179461-52-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 44 mg/mL (185.5 mM) Ethanol: 44 mg/mL (185.5 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Wang KK, et al. Proc Natl Acad Sci U S A. 1996, 93(13), 6687-6692. 2. Pörn-Ares MI, et al. Biochem J. 2003 Sep 1;374(Pt 2):403-11. |