Home>>Signaling Pathways>> GPCR/G protein>> GHSR>>PF-5190457
PF-5190457 Catalog No.GC31478

Size Price Stock Qty
5mg
$324.00
In stock
10mg
$510.00
In stock
25mg
$918.00
In stock
50mg
$1,530.00
In stock
100mg
$2,086.00
In stock

Customer Review

Based on customer reviews.

Tel: (626) 353-8530 Email: sales@glpbio.com

Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

View current batch:

Protocol

Cell experiment:

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:

[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.

Chemical Properties

Cas No. 1334782-79-4 SDF Download SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES CC1=NC=NC(C2=CC(CC[C@H]3N4CC5(CCN(C(CC6=CN7C=C(C)SC7=N6)=O)CC5)C4)=C3C=C2)=C1
Formula C29H32N6OS M.Wt 512.67
Solubility DMSO: 250 mg/mL (487.64 mM) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
  • Molarity Calculator

  • Dilution Calculator

Mass
=
Concentration
x
Volume
x
MW*
 
 
 
**When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / CoA (available online).

Calculate

Background

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

PF-5190457 has a superior balance of ghrelin receptor pharmacology and off-target selectivity[1].

PF-5190457 has excellent selectivity and demonstrates robust increases in glucose-stimulated insulin secretion in human whole and dispersed islets[1].

[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.