1. Membrane Transporter/Ion Channel
  2. P2X Receptor

CE-224535 (Synonyms: PF-04905428)

Cat. No.: HY-15487
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

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1 mg USD 2066 Get quote
5 mg USD 3306 Get quote
10 mg USD 5290 Get quote

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

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].

Clinical Trial
References
Molecular Weight

480.94

Formula

C₂₂H₂₉ClN₄O₆

CAS No.

724424-43-5

SMILES

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

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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CE-224535
Cat. No.:
HY-15487
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