2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. PF-07054894

PF-07054894 is an orally active and potent C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) antagonist that blocks CCR6-mediated chemotaxis with an IC50 value of 5.7 nM in vitro. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease.

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

PF-07054894 Chemical Structure

PF-07054894 Chemical Structure

CAS No. : 2413693-96-4

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Based on 1 publication(s) in Google Scholar

PF-07054894 Related Antibodies

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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Description

PF-07054894 is an orally active and potent C-C Chemoattractant Cytokine (Chemokine) Receptor 6 (CCR6) antagonist that blocks CCR6-mediated chemotaxis with an IC50 value of 5.7 nM in vitro. PF-07054894 targets G protein-coupled receptor (GPCR). PF-07054894 can be used in research of inflammatory bowel disease[1][2][3][4].

IC50 & Target[1]

CCR6

 

In Vitro

PF-07054894 (1-3000 nM, 1 h) inhibits CCL20/CCR6-mediated T Cell chemotaxis in an insurmountable manner[2].

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

PF-07054894 Related Antibodies
In Vivo

PF-07054894 (10 mg/kg, p.o., twice a day for 6 consecutive days) increases circulating CCR6+ T cells in naïve cynomolgus monkeys[2][3].
PF-07054894 (100 mg/kg, p.o., once or twice per day for 12 days) is efficacious in interleukin-23-induced inflammation in skin inflammation mouse model[2].

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

Animal Model: Naïve cynomolgus monkeys[2][3]
Dosage: 10 mg/kg
Administration: p.o., twice a day for 6 consecutive days
Result: Resulted in an increase in the frequency of most circulating CCR6+ T lymphocytes populations examined (CCR6+ CD4+ and CD8+ cells including total, effector, memory, Th17, and Th1/17 cells).
Animal Model: Skin inflammation mouse model[2]
Dosage: 100 mg/kg
Administration: p.o., once or twice per day for 12 days
Result: Inhibited mouse ear swelling induced by interleukin-23 intradermal injection.
Clinical Trial
Molecular Weight

466.53

Formula

C24H30N6O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OC1=C(C(N(C)C)=O)N=CC=C1NC2=C(N[C@@H](C3=NN(C)C=C3C)C4(C)CCCC4)C(C2=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (214.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1435 mL 10.7174 mL 21.4348 mL
5 mM 0.4287 mL 2.1435 mL 4.2870 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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
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Volume
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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% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.36 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

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
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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1435 mL 10.7174 mL 21.4348 mL 53.5871 mL
5 mM 0.4287 mL 2.1435 mL 4.2870 mL 10.7174 mL
10 mM 0.2143 mL 1.0717 mL 2.1435 mL 5.3587 mL
15 mM 0.1429 mL 0.7145 mL 1.4290 mL 3.5725 mL
20 mM 0.1072 mL 0.5359 mL 1.0717 mL 2.6794 mL
25 mM 0.0857 mL 0.4287 mL 0.8574 mL 2.1435 mL
30 mM 0.0714 mL 0.3572 mL 0.7145 mL 1.7862 mL
40 mM 0.0536 mL 0.2679 mL 0.5359 mL 1.3397 mL
50 mM 0.0429 mL 0.2143 mL 0.4287 mL 1.0717 mL
60 mM 0.0357 mL 0.1786 mL 0.3572 mL 0.8931 mL
80 mM 0.0268 mL 0.1340 mL 0.2679 mL 0.6698 mL
100 mM 0.0214 mL 0.1072 mL 0.2143 mL 0.5359 mL
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PF-07054894 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-070548942413693-96-4PF07054894PF 07054894CCRCC chemokine receptorG protein-coupled receptorinflammatorybowelInhibitorinhibitorinhibit

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