| Identification | Back Directory | [Name]
(R)-2-CHLORO-5-(4-(HYDROXY(METHOXY)METHYL)-3,5-DIOXO-4,5-DIHYDRO-1,2,4-TRIAZIN-2(3H)-YL)-N-((1-HYDROXYCYCLOHEPTYL)METHYL)BENZAMIDE | [CAS]
724424-43-5 | [Synonyms]
CE 224535
PF-04905428
A P2X7 receptor antagonist
inhibit,P2XRs,Inhibitor,CE 224535,PF04905428,P2X Receptor,CE-224535,PF 04905428,CE224535
2-CHLORO-N-[(1-HYDROXYCYCLOHEPTYL)METHYL]-5-[4-[(2R)-2-HYDROXY-3-METHOXYPROPYL]-3,5-DIOXO-1,2,4-TRIAZIN-2-YL]BENZAMIDE
(R)-2-CHLORO-5-(4-(HYDROXY(METHOXY)METHYL)-3,5-DIOXO-4,5-DIHYDRO-1,2,4-TRIAZIN-2(3H)-YL)-N-((1-HYDROXYCYCLOHEPTYL)METHYL)BENZAMIDE
Benzamide, 2-chloro-5-[4,5-dihydro-4-[(2R)-2-hydroxy-3-methoxypropyl]-3,5-dioxo-1,2,4-triazin-2(3H)-yl]-N-[(1-hydroxycycloheptyl)methyl]- | [Molecular Formula]
C22H29ClN4O6 | [MDL Number]
MFCD10698778 | [MOL File]
724424-43-5.mol | [Molecular Weight]
480.94 |
| Chemical Properties | Back Directory | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
13.48±0.20(Predicted) | [color ]
White to yellow |
| Hazard Information | Back Directory | [Uses]
CE-224535, is a selective P2X7 receptor antagonist. | [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]. | [IC 50]
P2X7 Receptor |
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