| Bioactivity | PF-5190457 (PF-05190457) is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36[1]. | ||||||||||||
| Target | pKi: 8.36 (Humnan ghrelin receptor) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | PF-5190457 | ||||||||||||
| CAS | 1334782-79-4 | ||||||||||||
| Formula | C29H32N6OS | ||||||||||||
| Molar Mass | 512.67 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |