| Description | LOC14 to be the most potent PDI inhibitor reported to date( EC50 : 500 nM) |
| In vitro | LOC14引起的PDI氧化，在细胞培养中不仅具有神经保护作用，而且在皮质纹状体脑片培养中也表现出同样效果[1]。 |
| In vivo | LOC14 在肝微粒体和血浆中显示出高稳定性，小鼠以高剂量20 mg/kg耐受良好，并能够在体内穿透血脑屏障(BBB)[1][2]。 |
| Animal experiments | LOC14 levels were measured in mouse plasma, striatum and cerebral cortex using Ultra Performance Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS).?LOC14 was extracted from mouse plasma by mixing 100 μl of plasma with 900 μl of cold acetonitrile containing 25 ng/ml of cyclocreatine as an internal standard.?After mixing for 5 min. the sample was centrifuged for 10min and the organic layer was transferred to an LC-MS vial and dried under nitrogen.?The sample was reconstituted in 100 μl of 50% acetonitrile and 5 μl was injected onto the LC-MS.?Brain tissue samples were homogenized using a tissue tearor at a concentration of 150 mg/ml in cold LC-MS water followed by extraction with 1.8 ml of cold acetonitrile containing the cyclocreatine internal standard.?The brain samples were mixed and centrifuged and reconstituted the same as for the plasma samples[2]. |
| Target activity | PDI:500 nM(EC50) |
| molecular weight | 317.41 |
| Molecular formula | C16H19N3O2S |
| CAS | 877963-94-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 25 mg/mL (78.76 mM) |
| References | 1. Kaplan A, et al. Small molecule-induced oxidation of protein disulfide isomerase is neuroprotective. Proc Natl Acad Sci U S A. 2015 Apr 28;112(17):E2245-52. 2. Zhou X , Li G , Kaplan A , et al. Small molecule modulator of protein disulfide isomerase attenuates mutant huntingtin toxicity and inhibits endoplasmic reticulum stress in a mouse model of Huntington’s disease[J]. Human Molecular Genetics, 2018. |
| Citations | 7. Yang M, Li Q, Yang H, et al.Downregulation of PDIA3 inhibits gastric cancer cell growth through cell cycle regulation.Biomedicine & Pharmacotherapy.2024, 173: 116336. |