产品
编 号：F620674
分子式：C29H42F3N5O7
分子量：629.67
分子式：C29H42F3N5O7
分子量：629.67
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CAS No: 2140301-98-8
产品详情
生物活性：
PF-0463481 succinate is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy.
体内研究：
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.Animal Model:Nos3-/- mice on the C57BL/6 background
Dosage:30 mg/kg
Administration:Oral administration; once daily; 31 days intervention (weeks 2-15) after Streptozotocin
Result:Had no impact on the fasting blood glucose levels, but induced an additional increase in HbA1c levels
PF-0463481 succinate is a potent and orally active dual CCR2/CCR5 antagonist with comparable human and rodent CCR2 potency (rat IC50=20.8 nM), and displays 10-20 fold less rodent CCR5 potency (rat IC50=470 nM). PF-0463481 succinate is safe and well-tolerated and has the potential for the study of diabetic nephropathy.
体内研究：
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.Animal Model:Nos3-/- mice on the C57BL/6 background
Dosage:30 mg/kg
Administration:Oral administration; once daily; 31 days intervention (weeks 2-15) after Streptozotocin
Result:Had no impact on the fasting blood glucose levels, but induced an additional increase in HbA1c levels
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