CE-224535

Research use only, not for human use.

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

CE-224535 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.(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).

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).

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.

PF-04905428

Membrane Transporter/Ion Channel

P2X Receptor

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724424-43-5

480.95

C22H29ClN4O6

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (207.93 mM)

COC[C@H](O)Cn1c(=O)cnn(-c2ccc(Cl)c(c2)C(=O)NCC2(O)CCCCCC2)c1=O

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(-20℃)

With Ice Pack

≥ 2 years