877963-94-5
877963-94-5 structure
- Name: LOC-14
- Chemical Name: LOC14
- CAS Number: 877963-94-5
- Molecular Formula: C16H19N3O2S
- Molecular Weight: 317.41
- Catalog: Research Areas Inflammation/Immunology
- Create Date: 2019-09-10 10:02:48
- Modify Date: 2025-09-18 17:05:49
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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].
| Name | LOC14 |
|---|
| 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]. |
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| Related Catalog | |
| 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. |
| References |
| Molecular Formula | C16H19N3O2S |
|---|---|
| Molecular Weight | 317.41 |