MK-0812 is a small molecule CCR2 antagonist. MK-0812 selectively reduced the peripheral blood monocyte frequency, and caused an elevation in the CCR2 ligand CCL2.
|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.
Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis.
Min SH, et al. Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6. PMID: 20004647.
Assessment of chemokine receptor function on monocytes in whole blood: In vitro and ex vivo evaluations of a CCR2 antagonist.
Wisniewski T, et al. J Immunol Methods. 2010 Jan 31;352(1-2):101-10. PMID: 19913021.
|Related CCR Products|
INCB 3284 is a potent, selective and orally bioavailable hCCR2 antagonist with IC50 of 3.7 nM.
Vicriviroc (SCH 417690) is a pyrimidine CCR5 entry inhibitor of HIV-1 with IC50 of 0.91 nM.
Maraviroc (UK-427857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity and favorable pharmacological properties.
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