CCX140 potently inhibits CCL2-induced chemotaxis of purified human blood monocytes with IC50 values of 8 nM in buffer and 200 nM in the presence of 100% human serum. CCX140-B also inhibits CCL2-induced Ca2+ mobilization in monocytes with an IC50 value of 3 nM. CCX140-B has a Kd value of 2.3 nM toward hCCR2.
In vivo, CCX140-B(100 mg/kg) treatment in DIO hCCR2 KI mice blocks the progressive increase in UAER and ACR. CCX140-B maintains lower UAER and ACR values during the entire 8-wk dosing regimen.
|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 10 mM|
CCR2 antagonist CCX140-B provides renal and glycemic benefits in diabetic transgenic human CCR2 knockin mice.
Sullivan T, et al. Am J Physiol Renal Physiol. 2013 Nov 1;305(9):F1288-97. PMID: 23986513.
Experimental evidence for the use of CCR2 antagonists in the treatment of type 2 diabetes.
Sullivan TJ, et al. Metabolism. 2013 Nov;62(11):1623-32. PMID: 23953944.
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