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INCB3344

Cat. No. M13926
INCB3344 Structure
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Biological Activity

INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.

Chemical Information
Molecular Weight 577.59
CAS Number 1262238-11-8
Solubility (25°C) DMSO 150 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Xin Tan, et al. Role of CCR2 in the Development of Streptozotocin-Treated Diabetic Cardiomyopathy

[2] Ping Xie, et al. Suppression and regression of choroidal neovascularization in mice by a novel CCR2 antagonist, INCB3344

[3] Chu-Biao Xue, et al. Discovery of INCB3344, a potent, selective and orally bioavailable antagonist of human and murine CCR2

[4] Niu Shin, et al. Pharmacological characterization of INCB3344, a small molecule antagonist of human CCR2

[5] Carrie M Brodmerkel, et al. Discovery and pharmacological characterization of a novel rodent-active CCR2 antagonist, INCB3344

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