1. GPCR/G Protein
  2. GHSR
  3. PF-5190457

PF-5190457 

Cat. No.: HY-12584
Handling Instructions

PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.

For research use only. We do not sell to patients.

PF-5190457 Chemical Structure

PF-5190457 Chemical Structure

CAS No. : 1334782-79-4

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Description

PF-5190457 is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36.

IC50 & 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].

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

512.67

Formula

C₂₉H₃₂N₆OS

CAS No.

1334782-79-4

SMILES

CC1=NC=NC(C2=CC(CC[[email protected]]3N4CC5(CCN(C(CC6=CN7C=C(C)SC7=N6)=O)CC5)C4)=C3C=C2)=C1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PF-5190457
Cat. No.:
HY-12584
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PF-5190457

Cat. No.: HY-12584