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

PF-04634817 

Cat. No.: HY-117621
COA 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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Other Forms of PF-04634817:

PF-04634817 Related Antibodies

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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

Appearance

Solid

Formula

C25H36F3N5O3
CAS No.
SMILES

O=C(N1[C@@]2([H])C[C@@]([H])(C1)N(C3=NC=NC(C(F)(F)F)=C3)C2)[C@@]4(C[C@@H](CC4)N[C@@H]5[C@@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 available by MedChemExpress (MCE).
Purity & Documentation
References
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PF-04634817 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

PF-046348171228111-63-4PF04634817PF 04634817CCRCC chemokine receptorDiabeticMacularEdemaOvertNephropathynon-alcoholicsteatohepatitisNASHfibrosisinterventionagentInhibitorinhibitorinhibit

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