| 产品描述: | 高亲和力蛋白质二硫键异构酶(PDI)调节剂;High affinity protein disulfide isomerase (PDI) modulator;产品介绍:LOC14 是蛋白质二硫键异构酶 (PDI) 抑制剂 (EC50=500 nM; Kd=62 nM)。LOC14 在小鼠肝微粒体和血浆中表现出高稳定性,低内在微粒体清除率和低血浆蛋白结合。LOC14 抑制 PDIA3 活性,降低肺上皮细胞中 HA 的分子内二硫键和随后的寡聚化。; |
| 靶点: |
Kd: 62 nM (PDI) |
| 体内研究: |
LOC14 (灌胃口服给药;20 mg/kg;每日一次;12-28 周) 显著改善 N171–82Q HD 小鼠的运动功能,减轻脑萎缩并延长生存期。 |
| 参考文献: |
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. Chamberlain N, et al. Lung epithelial protein disulfide isomerase A3 (PDIA3) plays an important role in influenza infection, inflammation, and airway mechanics. Redox Biol. 2019 Apr;22:101129. 3. Zhou X, 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. Hum Mol Genet. 2018 May 1;27(9):1545-1555. |
| 保存条件: |
避光,-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.15 ml |
15.752 ml |
31.505 ml |
| 5 mM |
0.63 ml |
3.15 ml |
6.301 ml |
| 10 mM |
0.315 ml |
1.575 ml |
3.15 ml |
| 50 mM |
0.063 ml |
0.315 ml |
0.63 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |