LOC14 is a potent PDI (protein disulfide isomerase) inhibitor with EC50 value of 500 nM. LOC14 has a Kd value of 62 nM. LOC14 inhibits PDIA3 activity, it also decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells.
In vivo, LOC14 (20 mg/kg/day; gavage; 12-28 weeks) significantly improves motor function, attenuated brain atrophy and extended survival in the N171–82Q HD mice.
| Molecular Weight | 317.41 |
| Formula | C16H19N3O2S |
| CAS Number | 877963-94-5 |
| Solubility (25°C) | DMSO ≥ 25 mg/mL |
| Storage | 2-8°C, protect from light, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related PDI Products |
|---|
| G6PDi-1
G6PDi-1 is a reversible and non-competitive glucose-6-phosphate dehydrogenase (G6PD) inhibitor with an IC50 of 0.07 μM. G6PDi-1 depletes NADPH most strongly in lymphocytes. G6PDi-1 markedly decreases inflammatory cytokine production in T cells. |
| ML359
ML359 is a potent, selctive and reversible inhibitor of protein disulfide isomerase (PDI), with an IC50 of 250 nM. ML359 can prevent thrombus formation in vivo. |
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