PF-0463481 succinate is a potent and orally active dualCCR2/CCR5antagonist with comparable human and rodentCCR2potency (ratIC₅₀=20.8 nM), and displays 10-20 fold less rodentCCR5potency (ratIC₅₀=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy^[3].

PF-04634817 succinate (oral administration; 30 mg/kg; once daily; 31 days intervention (weeks 2-15 after Streptozotocin )) intervention at the onset of diabetes (week 2) has no impact on the fasting blood glucose levels in diabetic Nos3^-/-221 mice. The development of diabetes results in a marked increase in the levels of glycated haemoglobin (HbA1c) in Nos3^-/-mice. Early intervention with PF-04634817 induces an additional increase in glycated hemoglobin (HbA1c) levels^[1].

629.67

Solid

C₂₉H₄₂F₃N₅O₇

2140301-98-8

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)