| Description |
PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.
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| Related Catalog |
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| Target |
pKi: 8.36 (Humnan ghrelin receptor)[1]
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| In Vitro |
PF-5190457 has a superior balance of ghrelin receptor pharmacology and off-target selectivity[1].
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| In Vivo |
PF-5190457 has excellent selectivity and demonstrates robust increases in glucose-stimulated insulin secretion in human whole and dispersed islets[1].
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| 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].
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| 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.
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