| Description | Varespladib (LY315920), a specific and effective human non-pancreatic secretory phospholipase A2 (hnsPLA) inhibitor(IC50=7 nM), has been investigated for the treatment and prevention of sickle cell disease, vaso-occlusive crisis, and acute coronary syndrome. |
| In vitro | 在表达人类sPLA2的转基因小鼠中,口服或静脉注射给药LY315920（0.3-3 mg/kg ）能够以剂量依赖的方式抑制血清sPLA2活性. |
| In vivo | 在缺少人类 sPLA2的BAL细胞中, LY315920（0.1 μM-3 μM）能够以浓度依赖的方式降低人类sPLA2调节的血栓形成。在人结膜上皮细胞系中,LY315920（10 μM ）显著抑制全－反式－维甲酸(RA)诱导的膜相关粘蛋白MUC16表达。在多种动物的血清中,LY315920明显抑制sPLA2活性,分别为大鼠（IC50=8.1 nM）、兔（IC50=5.0 nM）、豚鼠（IC50=3.2 nM）、人类的血清（IC50=6.2 nM）。 |
| Target activity | hnsPLA2:7 nM |
| Synonyms | LY315920, 伐瑞拉地, 伐瑞拉迪 |
| molecular weight | 380.39 |
| Molecular formula | C21H20N2O5 |
| CAS | 172732-68-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 60 mg/mL (157.73 mM), Sonication is recommended. Ethanol: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Draheim SE, et al. J Med Chem. 1996, 39(26), 5159-5175. 2. Snyder DW, et al. J Pharmacol Exp Ther. 1999, 288(3), 1117-1124. 3. Hori Y, et al. Invest Ophthalmol Vis Sci. 2005, 46(11), 4050-4061. |
| Citations | 1. Tan C H, Lingam T M C, Tan K Y. Varespladib (LY315920) rescued mice from fatal neurotoxicity caused by venoms of five major Asiatic kraits (Bungarus spp.) in an experimental envenoming and rescue model. Acta Tropica. 2021: 106289. |