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BioChemicals
CE-224535
tcsc0006791
CE-224535
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AVAILABLE SIZES
1mg
5mg
10mg
$
2,951.00
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ORDERING INFORMATION
International
TAICLONE BIOTECH CORP.
order@taiclone.com
+886-2-2735-9682
+886-2-2735-9807
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Product Description
CE-224535 is a selective
P2X
7
receptor
antagonist.
IC50 & Target: P2X
7
receptor
[1]
In Vitro:
CE-224535 is developed as a disease-modifying antirheumatic drugs (DMARD) and is a selective antagonist of the human P2X
7
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 CL
p
(11 mL/min/kg) and a large V
dss
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 (C
max
) that is ~90 fold over its IC
90
in human blood (C
max
=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]
.
Information
CAS No
724424-43-5
Formula
C
22
H
29
ClN
4
O
6
Clinical Information
clinicalinformation
Pathway
Membrane Transporter/Ion Channel
Target
P2X Receptor
Specifications
Purity / Grade
>98%
Solubility
10 mM in DMSO
Smiles
smiles
Misc Information
Alternative Names
PF-04905428
Observed Molecular Weight
480.94
related data
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