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LOC14 

Cat. No.: HY-100432
Handling Instructions

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.

For research use only. We do not sell to patients.

LOC14 Chemical Structure

LOC14 Chemical Structure

CAS No. : 877963-94-5

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Description

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[1]. LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells[3].

IC50 & Target

Kd: 62 nM (PDI)[1]

In Vitro

LOC14 (0.01-100 μM; 24 hours) exhibits the capacity to inhibit recombinant (r)PDIA3 at an IC50 of approximately 5 μM[3].

Cell Viability Assay[3]

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.
In Vivo

LOC14 (orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks) significantly improves motor function, attenuated brain atrophy and extended survival in the N171–82Q HD mice[2].

Animal Model: Male N171–82Q HD mice[2]
Dosage: 20 mg/kg
Administration: Orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks
Result: Improved motor function in HD mice.
Molecular Weight

317.41

Formula

C₁₆H₁₉N₃O₂S

CAS No.

877963-94-5

SMILES

O=C(C(C=CC=C1)=C1S2)N2CN3CCN(C(C4CC4)=O)CC3

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (78.76 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1505 mL 15.7525 mL 31.5050 mL
5 mM 0.6301 mL 3.1505 mL 6.3010 mL
10 mM 0.3150 mL 1.5752 mL 3.1505 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.55 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.55 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.55 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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LOC14
Cat. No.:
HY-100432
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