Ki16425 is an antagonist of the lysophosphatidic acid receptors LPA1 and LPA3. Ki16425 inhibits the LPA-induced Ca(2+) response in THP-1 cells, 3T3 fibroblasts and A431 cells. Ki16425 also inhibited LPA-induced long-term responses, including DNA synthesis and cell migration. Ki16425 reduced the LPA-induced activation of p42/p44 mitogen activated protein kinase (MAPK), while acting as a weak stimulator of p42/p44 MAPK on its own, properties typical of a protean agonist. Significantly, Ki16425 also reduced the NGF-induced stimulation of p42/p44 MAPK and inhibited NGF-stimulated neurite outgrowth.
|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||DMSO 90 mg/mL|
Protean agonism of the lysophosphatidic acid receptor-1 with Ki16425 reduces nerve growth factor-induced neurite outgrowth in pheochromocytoma 12 cells.
Moughal NA, et al. J Neurochem. 2006 Sep;98(6):1920-9. PMID: 16945108.
Ki16425, a subtype-selective antagonist for EDG-family lysophosphatidic acid receptors.
Ohta H, et al. Mol Pharmacol. 2003 Oct;64(4):994-1005. PMID: 14500756.
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