• 产品描述： LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding. LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells

• 靶点： Kd: 62 nM (PDI)

• 体外研究：
  LOC14 (0.01-100 μM；24 小时) 表现出抑制重组 (r) PDIA3 的能力，IC50 约为 5 μM。 Cell Viability Assay Cell Line: MTEC cells Concentration: 0.01 μM; 0.1 μM; 0.5 μM; 1 μM; 5 μM; 10 μM; 100 μM Incubation Time: 24 hours Result: Inhibited recombinant (r)PDIA3 activity.

• 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。 Animal Model: Male N171–82Q HD mice Dosage: 20 mg/kg Administration: Orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks Result: Improved motor function in HD mice.

• 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.

• 溶解性： Soluble  in  DMSO

• 保存条件： 2-8℃

• 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。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *