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

PF-4136309  (Synonyms: INCB8761)

Cat. No.: HY-13245 Purity: 99.18%
COA Handling Instructions

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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

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 110 In-stock
Solution
10 mM * 1 mL in DMSO USD 110 In-stock
Solid
5 mg USD 88 In-stock
10 mg USD 149 In-stock
50 mg USD 440 In-stock
100 mg USD 836 In-stock
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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of PF-4136309:

PF-4136309 Related Antibodies

Top Publications Citing Use of Products

2 Publications Citing Use of MCE PF-4136309

Cell Viability Assay

    PF-4136309 purchased from MedChemExpress. Usage Cited in: Materials Today. 2022.

    PGEM/PF-4136309 (PF) micelles exhibits potent anti-tumor efficacy. Tumor growth curve after combination of GEM (20 mg/kg; i.v) and PF (10 mg/kg; i.v). PGEM, an ultrasmall prodrug polymeric carrier of Gemcitabine (GEM).

    View All CCR Isoform Specific Products:

    View All Isoforms
    CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    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].

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

    PF-4136309 Related Antibodies
    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].

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

    568.59

    Formula

    C29H31F3N6O3
    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O[C@]1(CC[C@](CC1)([H])N[C@@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 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    Ethanol : 133.33 mg/mL (234.49 mM; Need ultrasonic)

    DMSO : ≥ 34 mg/mL (59.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (8.79 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 5 mg/mL (8.79 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  0.5% Methylcellulose/saline water

      Solubility: 10 mg/mL (17.59 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.59%

    COA (251 KB) HNMR (220 KB) LCMS (311 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 1 mM 1.7587 mL 8.7937 mL 17.5874 mL 43.9684 mL
    5 mM 0.3517 mL 1.7587 mL 3.5175 mL 8.7937 mL
    10 mM 0.1759 mL 0.8794 mL 1.7587 mL 4.3968 mL
    15 mM 0.1172 mL 0.5862 mL 1.1725 mL 2.9312 mL
    20 mM 0.0879 mL 0.4397 mL 0.8794 mL 2.1984 mL
    25 mM 0.0703 mL 0.3517 mL 0.7035 mL 1.7587 mL
    30 mM 0.0586 mL 0.2931 mL 0.5862 mL 1.4656 mL
    40 mM 0.0440 mL 0.2198 mL 0.4397 mL 1.0992 mL
    50 mM 0.0352 mL 0.1759 mL 0.3517 mL 0.8794 mL
    Ethanol 60 mM 0.0293 mL 0.1466 mL 0.2931 mL 0.7328 mL
    80 mM 0.0220 mL 0.1099 mL 0.2198 mL 0.5496 mL
    100 mM 0.0176 mL 0.0879 mL 0.1759 mL 0.4397 mL
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    PF-4136309 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.

    Keywords:

    PF-41363091341224-83-6INCB8761PF4136309PF 4136309INCB 8761INCB-8761CCRCC chemokine receptorInhibitorinhibitorinhibit

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