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    Immunology/Inflammation
  2. CCR
  3. PF-04634817 succinate

PF-04634817 succinate 

Cat. No.: HY-117621A Purity: >99.0%
Handling Instructions

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.

For research use only. We do not sell to patients.

PF-04634817 succinate Chemical Structure

PF-04634817 succinate Chemical Structure

CAS No. : 2140301-98-8

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1 mg USD 190 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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[3].

IC50 & Target[1]

Rat CCR2

20.8 nM (IC50)

CCR5

470 nM (IC50)

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[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
Molecular Weight

629.67

Formula

C₂₉H₄₂F₃N₅O₇

CAS No.

2140301-98-8

SMILES

O=C(N1[[email protected]@]2([H])C[[email protected]@]([H])(C1)N(C3=NC=NC(C(F)(F)F)=C3)C2)[[email protected]@]4(C[[email protected]@H](CC4)N[[email protected]@H]5[[email protected]@H](COCC5)OC)C(C)C.OC(CCC(O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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Keywords:

PF-04634817PF04634817PF 04634817CCRCC chemokine receptorDiabeticMacularEdemaOvertNephropathynon-alcoholicsteatohepatitisNASH,fibrosis,interventionagentInhibitorinhibitorinhibit

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Product name:
PF-04634817 succinate
Cat. No.:
HY-117621A
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