1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. CE-224535

CE-224535  (Synonyms: PF-04905428)

Cat. No.: HY-15487 Purity: 98.02%
COA Handling Instructions

CE-224535 is a selective P2X7 receptor antagonist.

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

CE-224535 Chemical Structure

CE-224535 Chemical Structure

CAS No. : 724424-43-5

Size Price Stock Quantity
5 mg USD 650 In-stock
10 mg USD 980 In-stock
25 mg USD 2050 In-stock
50 mg USD 3300 In-stock
100 mg USD 5280 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CE-224535 is a selective P2X7 receptor antagonist.

IC50 & Target

P2X7 receptor[1]

In Vitro

CE-224535 is developed as a disease-modifying antirheumatic drugs (DMARD) and is a selective antagonist of the human P2X7 receptor. CE-224535 can reduce leukocyte secretion of IL-1 and IL-18, thereby providing a novel therapeutic approach for treatment of rheumatoid arthritis (RA)[1].

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

In Vivo

In rats, CE-224535 has low CLp (11 mL/min/kg) and a large Vdss of 7.6 L/kg, which results in a half-life of 2.4 h. Upon oral administration to rats at 5 mg/kg, CE-224535 provides maximal plasma exposure (Cmax) that is ~90 fold over its IC90 in human blood (Cmax=0.21 μg/mL or 0.44 μM). The oral bioavailability of CE-224535 is low in rats (F=2.6%), but this is believed to be a rat specific phenomenon since corresponding oral bioavailability in both dog (59%) and monkey (22%) is adequate[2].

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

Clinical Trial
Molecular Weight

480.94

Formula

C22H29ClN4O6

CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1N(C[C@@H](O)COC)C(N(C2=CC=C(Cl)C(C(NCC3(O)CCCCCC3)=O)=C2)N=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (207.93 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 2.0793 mL 10.3963 mL 20.7926 mL
5 mM 0.4159 mL 2.0793 mL 4.1585 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 (sealed storage, away from moisture). 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
×
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% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 10 mg/mL (20.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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: ≥ 10 mg/mL (20.79 mM); Clear solution

    This protocol yields a clear solution of ≥ 10 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (100.0 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 (sealed storage, away from moisture)

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: 98.88%

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 (sealed storage, away from moisture). 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 2.0793 mL 10.3963 mL 20.7926 mL 51.9815 mL
5 mM 0.4159 mL 2.0793 mL 4.1585 mL 10.3963 mL
10 mM 0.2079 mL 1.0396 mL 2.0793 mL 5.1982 mL
15 mM 0.1386 mL 0.6931 mL 1.3862 mL 3.4654 mL
20 mM 0.1040 mL 0.5198 mL 1.0396 mL 2.5991 mL
25 mM 0.0832 mL 0.4159 mL 0.8317 mL 2.0793 mL
30 mM 0.0693 mL 0.3465 mL 0.6931 mL 1.7327 mL
40 mM 0.0520 mL 0.2599 mL 0.5198 mL 1.2995 mL
50 mM 0.0416 mL 0.2079 mL 0.4159 mL 1.0396 mL
60 mM 0.0347 mL 0.1733 mL 0.3465 mL 0.8664 mL
80 mM 0.0260 mL 0.1300 mL 0.2599 mL 0.6498 mL
100 mM 0.0208 mL 0.1040 mL 0.2079 mL 0.5198 mL
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CE-224535 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.

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Product Name:
CE-224535
Cat. No.:
HY-15487
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