1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR
  3. PF-4136309

PF-4136309 (Synonyms: INCB8761)

Cat. No.: HY-13245 Purity: 99.59%
Handling Instructions

PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.

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

PF-4136309 Chemical Structure

PF-4136309 Chemical Structure

CAS No. : 1341224-83-6

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 100 In-stock
Estimated Time of Arrival: December 31
5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 135 In-stock
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50 mg USD 400 In-stock
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100 mg USD 760 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-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.

IC50 & Target[1]

Human CCR2

5.2 nM (IC50)

Mouse CCR2

13 nM (IC50)

Rat CCR2

17 nM (IC50)

In Vitro

PF-4136309 is potent in human chemotaxis activity (IC50=3.9 nM) and in the whole blood assay (IC50=19 nM), with IC50 of 16 and 2.8 nM in mouse and rat chemotaxis assays. PF-4136309 is potent in inhibiting CCR2 mediated signaling events such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation with IC50 values of 3.3 and 0.5 nM, respectively. In hERG patch clamp assay, PF-4136309 inhibits hERG potassium current with an IC50 of 20 μM. PF-4136309 is not a cytochrome P450 (CYP) inhibitor, with IC50 values of >30 μM against five major CYP isozymes CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Moreover, PF-4136309 is not a CYP inducer at concentrations up to 30 μM[1].

In Vivo

PF-4136309 (2 mg/kg) exhibits a moderate half-life in both species after iv administration (2.5 and 2.4 h). When administered orally, PF-4136309 (10 mg/kg) is absorbed rapidly, with peak concentration time (Tmax) at 1.2 h for rats and 0.25 h for dogs. A similar half-life is observed in both species between iv dosing and po dosing. PF-4136309 is well absorbed, with an oral bioavailability of 78% in both species[1].

Molecular Weight

568.59

Formula

C₂₉H₃₁F₃N₆O₃

CAS No.

1341224-83-6

SMILES

O[[email protected]]1(CC[[email protected]](CC1)([H])N[[email protected]@H]2CN(CC2)C(CNC(C3=CC=CC(C(F)(F)F)=C3)=O)=O)C4=NC=C(C=C4)C5=NC=CC=N5

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 : ≥ 34 mg/mL (59.80 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7587 mL 8.7937 mL 17.5874 mL
5 mM 0.3517 mL 1.7587 mL 3.5175 mL
10 mM 0.1759 mL 0.8794 mL 1.7587 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: ≥ 2.08 mg/mL (3.66 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.66 mM); Clear solution

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

Purity: 99.59%

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Keywords:

PF-4136309INCB8761PF4136309PF 4136309INCB 8761INCB-8761CCRCC chemokine receptorInhibitorinhibitorinhibit

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PF-4136309
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HY-13245
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