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PF-4136309

Name: PF-4136309
Brand: TargetMol
SKU: T3430
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T3430Cas No. 1341224-83-6

Alias PF 4136309, INCB8761

PF-4136309 (INCB8761) is a specific, effective, and orally bioavailable CCR2 antagonist.

PF-4136309

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Purity: 99.47%

Catalog No. T3430Alias PF 4136309, INCB8761Cas No. 1341224-83-6

PF-4136309 (INCB8761) is a specific, effective, and orally bioavailable CCR2 antagonist.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$31	In Stock	In Stock
5 mg	$68	In Stock	In Stock
10 mg	$113	In Stock	In Stock
25 mg	$196	In Stock	In Stock
50 mg	$322	In Stock	In Stock
100 mg	$455	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$85	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.47%

Appearance:Solid

Color:White to Yellow

Resource Download

COA LCMS HNMR

Product Introduction

PF-4136309 AI Summary

PF-4136309 exhibits a broad range of bioactivities. It shows oral bioavailability in both rat and dog models at 10 mg/kg and demonstrates pharmacokinetic properties such as half-life, volume of distribution, and clearance after intravenous administration. The compound inhibits multiple cytochrome P450 enzymes and displays significant activity on human ERG channels, CCR2 receptors, and has antagonist activity at rat and mouse CCR2 receptors. Additionally, PF-4136309 antagonizes CCR2 receptors in human whole blood and PBMC, displaces specific ligands from human CCR2 receptors, and displays binding affinity to rat and mouse CCR2 receptors. The compound has shown various pharmacokinetic values like Cmax, Tmax, and AUC in rat and dog models. In antiviral studies, PF-4136309 inhibits SARS-CoV-2 induced cytotoxicity in both Caco-2 and VERO-6 cells, though with varying degrees of inhibition. It also shows inhibitory activity against the SARS-CoV-2 3CL-Pro protease. Furthermore, the compound inhibits the human HDAC6 enzyme, though the degree of inhibition varies depending on the assay conditions. PF-4136309 affects cell viability across different cell lines, promoting growth in HEK293T cells while showing mixed effects in U2OS and human fibroblast cells. This compound also influences the thermal stability of different protein domains, either slightly increasing or decreasing their stability, suggesting specific bioactive interactions with these proteins. Additionally, it modulates beta-arrestin recruitment assays across various GPCR targets, demonstrating both inhibitory and activating effects on multiple receptors. Overall, PF-4136309 is a multifaceted molecule with significant implications for pharmacokinetics, enzyme inhibition, antiviral activity, cellular viability, protein stability, and receptor modulation..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	PF-4136309 (INCB8761) is a specific, effective, and orally bioavailable CCR2 antagonist.
Targets&IC50	CCR2 (rat):13 nM, CCR2 (mouse):17 nM, CCR2 (human):5.2 nM
Synonyms	PF 4136309, INCB8761

Chemical Properties

Molecular Weight	568.59
Formula	C₂₉H₃₁F₃N₆O₃
Cas No.	1341224-83-6
Smiles	[H][C@@]1(CC[C@](O)(CC1)c1ccc(cn1)-c1ncccn1)N[C@H]1CCN(C1)C(=O)CNC(=O)c1cccc(c1)C(F)(F)F
Relative Density.	1.40 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 100 mg/mL (175.87 mM), Sonication is recommended.

Ethanol: 100 mg/mL (175.87 mM), Sonication is recommended.

In Vivo Formulation

10% EtOH+40% PEG300+5% Tween-80+45% Saline: 10 mg/mL (17.59 mM), Suspension.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	1.7587 mL	8.7937 mL	17.5874 mL	87.9368 mL
5 mM	0.3517 mL	1.7587 mL	3.5175 mL	17.5874 mL
10 mM	0.1759 mL	0.8794 mL	1.7587 mL	8.7937 mL
20 mM	0.0879 mL	0.4397 mL	0.8794 mL	4.3968 mL
50 mM	0.0352 mL	0.1759 mL	0.3517 mL	1.7587 mL
100 mM	0.0176 mL	0.0879 mL	0.1759 mL	0.8794 mL

Calculator

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc