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CE-224535

Catalog No. T14920   CAS 724424-43-5
Synonyms: PF-04905428

CE-224535 (PF-04905428) is a selective antagonist of P2X7 receptor. CE-224535 can be used in disease-modifying antirheumatic studies.

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CE-224535 Chemical Structure
CE-224535, CAS 724424-43-5
Pack Size Availability Price/USD Quantity
1 mg In stock $ 213.00
5 mg In stock $ 537.00
10 mg In stock $ 775.00
25 mg In stock $ 1,190.00
50 mg In stock $ 1,590.00
100 mg In stock $ 2,170.00
500 mg In stock $ 4,350.00
1 mL * 10 mM (in DMSO) In stock $ 413.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description CE-224535 (PF-04905428) is a selective antagonist of P2X7 receptor. CE-224535 can be used in disease-modifying antirheumatic studies.
In vitro CE-224535 reduces leukocyte secretion of IL-1 and IL-18, thereby providing a novel therapeutic approach for the treatment of rheumatoid arthritis[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. CE-224535 (5 mg/kg;oral) provides Cmax that is ~90 fold over its IC90 in human blood (0.21 μg/mL or 0.44 μM)[2].
Synonyms PF-04905428
Molecular Weight 480.94
Formula C22H29ClN4O6
CAS No. 724424-43-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 95 mg/mL (197.53 mM), sonification is recommended.

TargetMolReferences and Literature

1. Stock TC, et al. Efficacy and safety of CE-224,535, an antagonist of P2X7 receptor, in treatment of patients with rheumatoid arthritis inadequately controlled by methotrexate. J Rheumatol. 2012 Apr;39(4):720-7. 2. Duplantier AJ, et al. Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3708-11

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Clinical Compound Library Bioactive Compounds Library Max Inhibitor Library Neuronal Signaling Compound Library Bioactive Compound Library Anti-Cancer Compound Library Drug Repurposing Compound Library

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Keywords

CE-224535 724424-43-5 Membrane transporter/Ion channel Neuroscience P2X Receptor inhibit PF-04905428 P2XRs Inhibitor PF04905428 PF 04905428 CE 224535 CE224535 inhibitor

 

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