Description
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.
Product information
CAS Number: 2140301-98-8
Molecular Weight: 629.67
Formula: C29H42F3N5O7
Chemical Name: (3S,4S)-3-methoxy-N-[(1R,3S)-3-(propan-2-yl)-3-[(1S,4S)-5-[6-(trifluoromethyl)pyrimidin-4-yl]-2,5-diazabicyclo[2.2.1]heptane-2-carbonyl]cyclopentyl]oxan-4-amine; butanedioic acid
Smiles: CC(C)[C@]1(C[C@@H](CC1)N[C@H]1CCOC[C@H]1OC)C(=O)N1C[C@@H]2C[C@H]1CN2C1=CC(=NC=N1)C(F)(F)F.OC(=O)CCC(O)=O
InChiKey: WRPPUEHVLSHXJG-HTQYHTRRSA-N
InChi: InChI=1S/C25H36F3N5O3.C4H6O4/c1-15(2)24(6-4-16(10-24)31-19-5-7-36-13-20(19)35-3)23(34)33-12-17-8-18(33)11-32(17)22-9-21(25(26,27)28)29-14-30-22;5-3(6)1-2-4(7)8/h9,14-20,31H,4-8,10-13H2,1-3H3;1-2H2,(H,5,6)(H,7,8)/t16-,17+,18+,19+,20-,24+;/m1./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vivo:
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.
Products are for research use only. Not for human use.
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