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Purity: ≥98%
LOC14 (LOC-14) is a protein disulfide isomerase (PDI) modulator with a high affinity (Kd = 62 nM). In addition to suppressing PDI's activity, it forces PDI to adopt an oxidized conformation. In mouse models of neurodegenerative diseases involving protein misfolding and in the brains of patients with these diseases, protein disulfide isomerase (PDI), a chaperone protein in the endoplasmic reticulum, is up-regulated. This explains why LOC14 is neuroprotective.
| Targets |
PDI (Kd = 62 nM)
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| ln Vitro |
LOC-14 (0.01-100 μM; 24 hours) exhibits the ability to inhibit recombinant (r)PDIA3 at an IC50 of about 5 μM.
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| ln Vivo |
LOC-14 (orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks) prolongs survival, attenuates brain atrophy, and significantly improves motor function in N171-82Q HD mice. Male N171-82Q HD mice are the animal model. 20 mg per kilogram. 20 mg/kg, given once daily, orally, for a period of 12 to 28 weeks. Improved motor performance in HD mice as a result. LOC14 was freshly made by first combining it with 1-Methyl-2-pyrrolidinone (NMP) to create an 80 mg/ml stock solution, and then diluting it with 0.5% methyl cellulose to the desired concentration (40× dilution).
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| Cell Assay |
Cells MTEC Concentration: 0.01 μM; 0.1 μM; 0.5 μM; 1 μM; 5 μM; 10 μM; 100 μM 24-hour incubation period; result: reduced activity of recombinant (r)PDIA3.
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| References |
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| Molecular Formula |
C16H19N3O2S
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|---|---|
| Molecular Weight |
317.41
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| Exact Mass |
317.12
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| Elemental Analysis |
C, 60.55; H, 6.03; N, 13.24; O, 10.08; S, 10.10
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| CAS # |
877963-94-5
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| Related CAS # |
877963-94-5
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| Appearance |
Solid powder
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| SMILES |
C1CC1C(=O)N2CCN(CC2)CN3C(=O)C4=CC=CC=C4S3
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| InChi Key |
YVBSNHLFRIVWFQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19N3O2S/c20-15(12-5-6-12)18-9-7-17(8-10-18)11-19-16(21)13-3-1-2-4-14(13)22-19/h1-4,12H,5-11H2
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| Chemical Name |
2-[[4-(cyclopropanecarbonyl)piperazin-1-yl]methyl]-1,2-benzothiazol-3-one
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| Synonyms |
LOC14; LOC 14; LOC-14
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~157.5 mM)
Water: ˂1 mg/mL Ethanol: ~19 mg/mL (~60 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.55 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.55 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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