BMS-570520 

BMS-570520 is an orally bioavailable CCR3 antagonist with an IC₅₀ of 1.9 nM against hCCR3 and an IC₅₀ of 1300 nM against hCYP2D6. BMS-570520 inhibits CYP2D6, but shows low activity against off-target G protein-coupled receptors, biogenic amine transporters, and the hERG potassium channel. BMS-570520 regulates chemotaxis, calcium mobilization, and anti-inflammatory pathways. BMS-570520 can be used in research related to asthma, allergic rhinitis, and contact dermatitis^[1].

BMS-570520 inhibits the binding of eotaxin to human CCR3 and mouse CCR3, with IC₅₀ values of 1.9 nM and 3.6 nM, respectively^[1].
BMS-570520 inhibits eotaxin-induced chemotaxis of human eosinophils or mouse eosinophils, with IC₅₀ values of 0.068 nM and 7 nM, respectively^[1].
BMS-570520 inhibits eosinophil chemokine-induced calcium mobilization via human CCR3, with an IC₅₀ of 2.6 nM^[1].
BMS-570520 exhibits off-target activity against human 5HT2A (IC₅₀=5300 nM), D2 (IC₅₀=640 nM), hERG (IC₅₀=6000 nM), serotonin transporter (K_i=29,000 nM), dopamine transporter (K_i=6500 nM), and norepinephrine transporter (K_i=7700 nM)^[1].
The apparent permeability coefficient of BMS-570520 in human Caco-2 cells is 2.8 × 10^-6 cm/s^[1].
BMS-570520 exhibits a protein binding rate of 93.1% in human serum and an intrinsic clearance of 0.96 L/h/kg in human liver microsomes^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

529.67

C₂₇H₃₆FN₅O₃S

388101-58-4

CC(C(SC(NC(N[C@H](CN(CC1)C(C)=O)[C@@H]1CN2C[C@@H](CCC2)CC3=CC=C(C=C3)F)=O)=N4)=C4C)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Pruitt JR, et al. CC chemokine receptor-3 (CCR3) antagonists: improving the selectivity of DPC168 by reducing central ring lipophilicity. Bioorg Med Chem Lett. 2007;17(11):2992-2997.  [Content Brief]