1. GPCR/G Protein
  2. GHSR

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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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9506 mL 9.7529 mL 19.5057 mL
5 mM 0.3901 mL 1.9506 mL 3.9011 mL
10 mM 0.1951 mL 0.9753 mL 1.9506 mL
*Please refer to the solubility information to select the appropriate solvent.
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.

Animal Administration

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

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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

PF-5190457

Cat. No.: HY-12584