[CAS NO. 724424-43-5] CE-224535

Name: CE-224535
Brand: Arctom Scientific
SKU: AS946949

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PRODUCTS SPECIFICATIONS [724424-43-5]

Distributor

Catalog

AS946949

Brand

Arctom Scientific

CAS

724424-43-5

DESCRIPTION [724424-43-5]

Overview

MDL	MFCD27665471
Molecular Weight	480.94
Molecular Formula	C22H29ClN4O6
SMILES	O=C1N(C[C@@H](O)COC)C(N(C2=CC=C(Cl)C(C(NCC3(O)CCCCCC3)=O)=C2)N=C1)=O

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

Summary

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] .

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

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] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00418782	Pfizer	Osteoarthritis	January 2007	Phase 2

Appearance

Solid

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)

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
10 mM	0.2079 mL	1.0396 mL	2.0793 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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
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
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.