LOC14

SKU: orb1301716

Description

LOC14 is the most potent small-molecule inhibitor of protein disulfide isomerase (PDI) currently reported, exhibiting an EC50 of 500 nM. This compound is a valuable research tool for investigating PDI's role in thrombus formation, cancer cell survival, and neurodegenerative diseases in both cellular and animal models.

Key Properties

• CAS Number: 877963-94-5
• MW: 317.41
• Purity: 99.62% (May vary between batches)
• Formula: C₁₆H₁₉N₃O₂S
• SMILES: O=C(C1CC1)N1CCN(Cn2sc3ccccc3c2=O)CC1
• Target: Others
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.3 mM);DMSO:50 mg/mL (157.52 mM)

Bioactivity

• Target IC50:
  PDI:500 nM(EC50)
• In Vivo:
  LOC14 showed high stability in liver microsomes and blood plasma, was tolerated at a high dose of 20 mg/kg in mice, and penetrated the BBB in vivo.
• In Vitro:
  LOC14-induced oxidation of PDI has a neuroprotective effect not only in cell culture, but also in corticostriatal brain slice cultures.
• Animal Research:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, LOC 14, LOC14, LOC-14, PDI

Compound Identifiers

PubChem CID

9117962