| Identification | Back Directory | [Name]
PF-4634817 | [CAS]
1228111-63-4 | [Synonyms]
PF-4634817
PF-04634817
D-erythro-Pentitol, 1,5-anhydro-2,3-dideoxy-4-O-methyl-3-[[(1R,3S)-3-(1-methylethyl)-3-[[(1S,4S)-5-[6-(trifluoromethyl)-4-pyrimidinyl]-2,5-diazabicyclo[2.2.1]hept-2-yl]carbonyl]cyclopentyl]amino]- | [Molecular Formula]
C25H36F3N5O3 | [MDL Number]
MFCD27987915 | [MOL File]
1228111-63-4.mol | [Molecular Weight]
511.58 |
| Chemical Properties | Back Directory | [Boiling point ]
630.3±55.0 °C(Predicted) | [density ]
1.30±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 50 mg/mL (97.74 mM) | [form ]
Solid | [pka]
8.62±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
PF-0463481 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 is safe and well-tolerated and has the potential for the study of diabetic nephropathy[3]. | [in vivo]
PF-04634817 (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]. | Animal Model: | Nos3-/- mice on the C57BL/6 background[1] | | 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. |
| [IC 50]
Rat CCR2: 20.8 nM (IC50); CCR5: 470 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Tesch GH, et al. Combined inhibition of CCR2 and ACE provides added protection against progression of diabetic nephropathy in?Nos3-deficient mice.Am J Physiol Renal Physiol.?2019 Dec 1;317(6):F1439-F1449. DOI:10.1152/ajprenal.00340.2019
[2] Gale JD, et al. A CCR2/5 Inhibitor, PF-04634817, Is Inferior to Monthly Ranibizumab in the Treatment of Diabetic Macular Edema. Invest Ophthalmol Vis Sci. 2018 May 1;59(6):2659-2669. DOI:10.1167/iovs.17-22731
[3] Gale JD, et al. Effect of PF-04634817, an Oral CCR2/5 Chemokine Receptor Antagonist, on Albuminuria in Adults with Overt Diabetic Nephropathy. Kidney Int Rep. 2018 Aug 3;3(6):1316-1327. DOI:10.1016/j.ekir.2018.07.010 |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 13348960310; |
| Website: |
https://www.weikeqi-biotech.com/ |
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