These renal pathological analyses showed that propacetamol injection induced AIKI in a subset of mice similar to those observed in APAP overdose patients.
|Cell lines||HEK 293 cells|
|Preparation method||To investigate whether PPCM exhibits hTRPV1-activating properties, HEK 293 cells expressing wild-type hTRPV1 were examined by standard whole-cell voltage clamp experiments. Measuring ramp currents by 500-millisecond depolarizations from −100 to +100 mV, we applied PPCM at increasing concentrations (1 µM to 10 mM).|
|Concentrations||1 µM to 10 mM|
|Incubation time||24 h|
|Animal models||Male 7-week-old BALB/c mice|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Propacetamol-Induced Injection Pain Is Associated with Activation of Transient Receptor Potential Vanilloid 1 Channels.
Schillers F, et al. J Pharmacol Exp Ther. 2016 Oct;359(1):18-25. PMID: 27457427.
Galangin Prevents Acute Hepatorenal Toxicity in Novel Propacetamol-Induced Acetaminophen-Overdosed Mice.
Tsai MS, et al. J Med Food. 2015 Nov;18(11):1187-97. PMID: 26501381.
LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
Compstatinis is a 13-residue cyclic peptide, binds to complement component C3 and inhibits complement activation with IC50 of 12 μM.
Azaserine is an inhibitor of the rate limiting step of the hexosamine biosynthethic pathway (HBP) and an irreversible inhibitor of GGT1 (gamma-Glutamyltranspeptidase).
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