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LOC14

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Chemical Structure| 877963-94-5 同义名 : -
CAS号 : 877963-94-5
货号 : A834854
分子式 : C16H19N3O2S
纯度 : 99%+
分子量 : 317.406
MDL号 : MFCD07849042
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(157.53 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 LOC14 is a strong inhibitor of Protein disulfide isomerase (PDI), displaying EC50 and Kd values of 500 nM and 62 nM, respectively. It demonstrates high stability in mouse liver microsomes and blood plasma, exhibits low clearance by microsomes, and has minimal binding to plasma proteins[1]. LOC14 suppresses the activity of PDIA3, leading to a reduction in intramolecular disulfide bonds and the subsequent oligomerization (maturation) of HA within lung epithelial cells. LOC14 demonstrates the ability to inhibit recombinant PDIA3, with an IC50 value around 5 μM when applied at concentrations ranging from 0.01 to 100 μM over a period of 24 hours[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.15mL

0.63mL

0.32mL

15.75mL

3.15mL

1.58mL

31.51mL

6.30mL

3.15mL
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]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.

[3]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.