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LOC14

Catalog No. T5534 CAS 877963-94-5

LOC14 to be the most potent PDI inhibitor reported to date( EC50 : 500 nM)

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LOC14, CAS 877963-94-5

Pack Size	Availability	Price/USD
5 mg	In stock	$ 43.00
10 mg	In stock	$ 81.00
25 mg	In stock	$ 171.00
50 mg	In stock	$ 310.00
100 mg	In stock	$ 543.00

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Purity: 98.22%

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Description	LOC14 to be the most potent PDI inhibitor reported to date( EC50 : 500 nM)
Targets&IC50	PDI:500 nM(EC50)
In vitro	LOC14-induced oxidation of PDI has a neuroprotective effect not only in cell culture, but also in corticostriatal brain slice cultures[1].
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[1][2].
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[2].

Molecular Weight	317.41
Formula	C16H19N3O2S
CAS No.	877963-94-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (78.76 mM)

References and Literature

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 , Li G , Kaplan A , 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[J]. Human Molecular Genetics, 2018.

Citations

7. Yang M, Li Q, Yang H, et al.Downregulation of PDIA3 inhibits gastric cancer cell growth through cell cycle regulation.Biomedicine & Pharmacotherapy.2024, 173: 116336.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library NO PAINS Compound Library Bioactive Compound Library Bioactive Compounds Library Max

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Keywords

LOC14 877963-94-5 Others LOC-14 inhibit LOC 14 Inhibitor inhibitor

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