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(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

Basic information Safety Supplier Related

(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 Basic information

Product 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
Synonyms:
  • (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
  • A P2X7 receptor antagonist
  • CE 224535
  • 2-CHLORO-N-[(1-HYDROXYCYCLOHEPTYL)METHYL]-5-[4-[(2R)-2-HYDROXY-3-METHOXYPROPYL]-3,5-DIOXO-1,2,4-TRIAZIN-2-YL]BENZAMIDE
  • PF-04905428
  • 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]-
  • inhibit,P2XRs,Inhibitor,CE 224535,PF04905428,P2X Receptor,CE-224535,PF 04905428,CE224535
  • CE-224535, 10 mM in DMSO
CAS:
724424-43-5
MF:
C22H29ClN4O6
MW:
480.94
Mol File:
724424-43-5.mol
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(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 Chemical Properties

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
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(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 Usage And Synthesis

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

(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)BENZAMIDESupplier

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Fan De(Beijing) Biotechnology Co., Ltd.
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(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(724424-43-5)Related Product Information