PD151746是有效的、选择性的钙蛋白酶抑制剂。PD151746抑制 u-calpain (Ki = 0.26 ± 0.03 μM) 选择性比抑制 m-calpain (Ki = 5.33 ± 0.77μM) 高20倍。

PD151746 is a calpain inhibitor that exhibits a 20-fold selectivity for u-calpain (Ki = 0.26 ± 0.03 μM) over m-calpain (Ki = 5.33 ± 0.77 μM). IC50 value: 0.26 ± 0.03 μM (Ki, for μ-calpain), 5.33 ± 0.77 μM (Ki, for m-calpain) [1] Target: calpain in vitro: The μ-calpain inhibitor PD 151746 decreases oxLDL-induced cytotoxicity. [2]

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。

Akt kinase assay: MM.1S cells are cultured in the presence or absence of perifosine (5 μM, 6 hours) and then stimulated with IL-6 (20 ng/mL, 10 minutes). In vitro akt kinase assay is then carried out using the Akt Kinase Assay Kit.

179461-52-0

C11H8FNO2S

237.25

H2O:<1 mgml
DMSO:44 mg/mL (185.5 mM)
Ethanol:44 mg/mL (185.5 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years