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.
NSC 23766 is an inhibitor of Rac GTPase targeting Rac activation by guanine nucleotide exchange factors (GEFs) with IC50 of ~50 μM in a cell-free assay; does not inhibit the closely related targets, Cdc42 or RhoA.
Budesonide is a GC steroid commonly used for the treatment of asthma and non-infectious rhinitis.
Brequinar is a potent inhibitor of dihydroorotate dehydrogenase, with potent activities against a broad spectrum of viruses.
Laropiprant is a potent, selective DP1 receptor antagonist with Ki value of 0.57 nM, and exhibits > 1,000 fold selectivity over DP2 receptor (Ki=0.75 μM).
Thiazolidinediones (TZDs) are peroxisome proliferator-activated receptor γ agonists that improve insulin-mediated glucose uptake and possess beneficial vasculoprotective actions.
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