Home Immunology & Inflammation CCR antagonist PF-4136309 For research use only.

PF-4136309

Synonyms: INCB8761, PF-04136309

PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2.

PF-4136309 Chemical Structure

PF-4136309 Chemical Structure

CAS No. 857679-55-1

Purity & Quality Control

Batch: S836101 DMSO]100 mg/mL]false]Ethanol]100 mg/mL]false]Water]Insoluble]false Purity: 99.60%
99.60

PF-4136309 Related Products

Signaling Pathway

CCR Signaling Pathways

CCR Signaling Pathway

Biological Activity

Description PF-4136309 (INCB8761, PF-04136309) is a potent, selective, and orally bioavailable CCR2 antagonist with an IC50 of 5.2 nM for human CCR2.
Targets
CCR2 [1]
5.2 nM
In vitro
In vitro

PF-4136309 is potent in inhibiting CCR2 mediated signaling events such as intracellular calcium mobilization and ERK (extracellular signal-regulated kinase) phosphorylation. <sup><a class="sref" href="#s_ref">[1]</a></sup>
Cell Research Cell lines Human PBMCs
Concentrations 0.001 μM –10 μM
Incubation Time 30 min
Method

500,000 HPBMCs in serum free DMEM media are incubated with or without PF-4136309 and warmed to 37 °C. 400 μL of warmed 10 nM MCP-1 is added to the bottom chamber in all wells except the negative control. An 8 micron membrane filter is placed on top and the chamber lid is closed. Cells are then added to the holes in the chamber lid which are associated with the chamber wells below the filter membrane. The whole chamber is incubated at 37 °C, 5% CO2 for 30 min. The cells are then aspirated off, the chamber lid opened, and the filter gently removed. The filter is air dried and stained with Wright Geimsa stain. Filters are counted by microscopy.  Antagonist potency is determined by comparing the number of cells that migrate to the bottom chamber in wells which contained antagonist, to the number of cells which migrate to the bottom chamber in MCP-1 control wells.
In Vivo
In vivo

PF-4136309 exhibits >100-fold selectivity over other homologous chemokine receptors, a free fraction of 24% in human serum and 15% in mouse serum, and an oral bioavailability of 47% in mice, suitable as a tool compound for target validation in rodent models.<sup><a class="sref" href="#s_ref">[2]</a></sup>
Animal Research Animal Models Rats, Dogs
Dosages 2 mg/kg
Administration I.v.

Chemical Information & Solubility

Molecular Weight 568.59 Formula

C29H31F3N6O3
CAS No. 857679-55-1 SDF --
Smiles OC1(CCC(CC1)NC2CCN(C2)C(=O)CNC(=O)C3=CC(=CC=C3)C(F)(F)F)C4=NC=C(C=C4)C5=NC=CC=N5
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (175.87 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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