1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR
  3. PF-04634817

PF-04634817 

Cat. No.: HY-117621 Purity: 98.87%
Handling Instructions

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.

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

PF-04634817 Chemical Structure

PF-04634817 Chemical Structure

CAS No. : 1228111-63-4

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1 mg USD 190 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 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].

IC50 & Target[1]

Rat CCR2

20.8 nM (IC50)

CCR5

470 nM (IC50)

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.
Clinical Trial
Molecular Weight

511.58

Formula

C₂₅H₃₆F₃N₅O₃

CAS No.

1228111-63-4

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

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
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (97.74 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9547 mL 9.7736 mL 19.5473 mL
5 mM 0.3909 mL 1.9547 mL 3.9095 mL
10 mM 0.1955 mL 0.9774 mL 1.9547 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.89 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.89 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.89 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PF-04634817PF04634817PF 04634817CCRCC chemokine receptorDiabeticMacularEdemaOvertNephropathynon-alcoholicsteatohepatitisNASHfibrosisinterventionagentInhibitorinhibitorinhibit

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Product Name:
PF-04634817
Cat. No.:
HY-117621
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