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1334782-79-4

1334782-79-4 structure
1334782-79-4 structure
  • Name: PF 05190457
  • Chemical Name: FF33NL9U5G
  • CAS Number: 1334782-79-4
  • Molecular Formula: C29H32N6OS
  • Molecular Weight: 512.669
  • Catalog: Signaling Pathways GPCR/G Protein GHSR
  • Create Date: 2018-07-08 06:28:14
  • Modify Date: 2024-01-02 13:22:19
  • PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.

Name FF33NL9U5G
Synonyms 2-(2-Methylimidazo[2,1-b][1,3]thiazol-6-yl)-1-{2-[(1R)-5-(6-methyl-4-pyrimidinyl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-yl}ethanone
PF-05190457
FF33NL9U5G
Ethanone, 1-[2-[(1R)-2,3-dihydro-5-(6-methyl-4-pyrimidinyl)-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-yl]-2-(2-methylimidazo[2,1-b]thiazol-6-yl)-
Description PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
Related Catalog
Target

pKi: 8.36 (Humnan ghrelin receptor)[1]

In Vitro PF-5190457 has a superior balance of ghrelin receptor pharmacology and off-target selectivity[1].
In Vivo PF-5190457 has excellent selectivity and demonstrates robust increases in glucose-stimulated insulin secretion in human whole and dispersed islets[1].
Cell Assay Human whole islets are incubated in assay buffer containing 2.8 mM glucose for 45 minutes at 37 °C to stabilize insulin secretion; islets are then treated with 11.2 mM glucose in the presence and absence of PF-5190457 for one hour at 37 °C. Following incubation, samples are tested for the amount of insulin secreted into the media[1].
References

[1]. Bhattacharya SK, et al. Discovery of PF-5190457, a Potent, Selective, and Orally Bioavailable Ghrelin Receptor Inverse Agonist Clinical Candidate. ACS Med Chem Lett. 2014 Feb 24;5(5):474-9.

Density 1.4±0.1 g/cm3
Molecular Formula C29H32N6OS
Molecular Weight 512.669
Exact Mass 512.235840
LogP 4.80
Index of Refraction 1.757
RIDADR NONH for all modes of transport