PF 05190457

Catalog #: 6350
1 Citation Datasheet / COA / SDS

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6350/25
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PF 05190457 | CAS No. 1334782-79-4 | Ghrelin Receptor Inverse Agonists

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Description: High affinity and selective ghrelin receptor inverse agonist

Chemical Name: 1-[2-[(1R)-2,3-Dihydro-5-(6-methyl-4-pyrimidinyl)-1H-inden-1-yl]-2,7-diazaspiro[3,5]non-7-yl]-2-(2-methylimidazo[2,1-b]thiazol-6-yl)ethanone

Purity: ≥98%

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Product Details

Citations (1)

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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

PF 05190457 is a high affinity and selective ghrelin receptor inverse agonist (K_d = 3 nM). Exhibits selectivity for ghrelin receptors over a panel of other targets. Increases intracellular Ca²⁺ concentration in and insulin secretion from human islets in vitro. Increases gastric afferent nerve activity in a rat ex vivo stomach preparation.

Technical Data

M.Wt:

512.67

Formula:

C₂₉H₃₂N₆O_S

Solubility:

Soluble to 5 mM in DMSO with gentle warming and to 10 mM in ethanol with gentle warming

Purity:

≥98%

Storage:

Store at -20°C

CAS No:

1334782-79-4

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:

Sold for research purposes under agreement from Pfizer Inc

Background References

Discovery of PF-5190457, a potent, selective, and orally bioavailable ghrelin receptor inverse agonist clinical candidate.
Bhattacharya et al.
ACS Med.Chem.Lett., 2014;5:474
Pharmacological characterization of the first in class clinical candidate PF-05190457: a selective ghrelin receptor competitive antagonist with inverse agonism that increases vagal afferent firing and glucose-dependent Ins secretion ex vivo.
Kong et al.
Br.J.Pharmacol., 2016;173:1452

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Citation for PF 05190457

The citations listed below are publications that use Tocris products. Selected citations for PF 05190457 include:

1 Citation: Showing 1 - 1

Molecular mechanism of agonism and inverse agonism in ghrelin receptor.
Authors: Chao Et al.
Nat Commun 2022;13:300

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