| Name | CAY10594 |
| Description | CAY10594 is a potent phospholipase D2(PLD2) inhibitor. CAY10594 ameliorates acetaminophen-induced acute liver injury by regulating the phosphorylated-GSK-3β/JNK axis. |
| Animal Research | Mice were fasted for 16?hours before APAP injection. APAP (500?mg/kg) was administered with oral gavage in mice. CAY10594 (N-[2-(4-oxo-1-phenyl-1,3,8-triazaspiro[4,5]dec-8-yl)ethyl]-2-naphthalene carboxamide)23 was dissolved in 1% DMSO and intraperitoneally administered to mice 30?minutes prior to APAP injection for examining protective effects or after 3?hours from APAP challenge for investigating therapeutic effects of CAY10594[1]. |
| In vivo | CAY10594 administration markedly blocked the acute liver injury in a dose-dependent manner, showing almost complete inhibition with 8?mg/kg of CAY10594. During the pathological progress of acute liver injury, GSH levels are decreased, and this is significantly recovered upon the administration of CAY10594 at 6?hours post APAP challenge. GSK-3β (Serine 9)/JNK phosphorylation is mainly involved in APAP-induced liver injury. CAY10594 administration strongly blocked GSK-3β (Serine 9)/JNK phosphorylation in the APAP-induced acute liver injury model. Consistently, sustained JNK activation in the cytosol and mitochondria from hepatocytes were also decreased in CAY10594-treated mice. Many types of immune cells are also implicated in APAP-induced liver injury. However, neutrophil and monocyte populations were not different between vehicle- and CAY10594-administered mice which are challenged with APAP. Therapeutic administration of CAY10594 also significantly attenuated liver damage caused by the APAP challenge, eliciting an enhanced survival rate[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 20 mg/mL (46.7 mM)
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| Keywords | Inhibitor | Phospholipase | CAY 10594 | CAY10594 | inhibit | CAY-10594 |
| Inhibitors Related | Neomycin sulfate | 1-Naphthaleneacetic acid potassium salt | trans-Benzylideneacetone | Benzylideneacetone | Tris(2,4-di-tert-butylphenyl)phosphate | (E/Z)-Polydatin | Indomethacin | Fluticasone (propionate) | 1-Naphthaleneacetic acid | Darapladib | Lansoprazole | Amentoflavone |
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United States
