Name | FF33NL9U5G |
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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. |
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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 |
Density | 1.4±0.1 g/cm3 |
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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 |
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