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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.
| Molecular Weight | 495.86 |
| Formula | C20H13ClF3N5O3S |
| CAS Number | 1100318-47-5 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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