PF 04628935

Names

[ Name ]:
PF 04628935

[Synonym ]:
1-{2-[2-Chloro-4-(2H-1,2,3-triazol-2-yl)benzyl]-2,7-diazaspiro[3.5]non-7-yl}-2-(2-methylimidazo[2,1-b][1,3]thiazol-6-yl)ethanone
Ethanone, 1-[2-[[2-chloro-4-(2H-1,2,3-triazol-2-yl)phenyl]methyl]-2,7-diazaspiro[3.5]non-7-yl]-2-(2-methylimidazo[2,1-b]thiazol-6-yl)-

Biological Activity

[Description]:

PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> GHSR

[Target]

GHSR1a:4.6 nM (IC50)

[References]

[1]. Kung DW, et, al. Identification of spirocyclic piperidine-azetidine inverse agonists of the ghrelin receptor. Bioorg Med Chem Lett. 2012 Jul 1;22(13):4281-7.

[2]. Cavalcante DP, et, al. Role of dorsal raphe nucleus GHS-R1a receptors in the regulation of inhibitory avoidance and escape behaviors in rats. Behav Brain Res. 2019 Jun 3;365:178-184.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₂₄H₂₆ClN₇OS

[ Molecular Weight ]:
496.03

[ Exact Mass ]:
495.160797

[ LogP ]:
4.14

[ Index of Refraction ]:
1.764

Safety Information

[ RIDADR ]:
NONH for all modes of transport

Related Compounds

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