INCB 3284 dimesylate exhibits potenct antagonism against monocyte chemoattractant molecule binding to hCCR2 and chemotaxis activity (IC50 values are 3.7 and 4.7 nM respectively). INCB 3284 also displays weak hERG activity; inhibits the hERG potassium current (IC50 = 84μM).
|Animal models||male C57Bl/6 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|
Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline
McMillin M, et al. J Neuroinflammation. 2014 Jul 10;11:121. PMID: 25012628.
Klotho gene deficiency causes salt-sensitive hypertension via monocyte chemotactic protein-1/CC chemokine receptor 2-mediated inflammation.
Zhou X, et al. J Am Soc Nephrol. 2015 Jan;26(1):121-32. PMID: 24904083.
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