YIL 781

Pricing Availability Delivery Time Qty
Cat.No. 3959 - YIL 781 | C24H28FN3O2.HCl | CAS No. 875258-85-8
Description: Ghrelin receptor (GHS-R1a) antagonist
Chemical Name: 6-(4-Fluorophenoxy)-2-methyl-3-[[(3S)-1-(1-methylethyl)-3-piperidinyl]methyl]-4(3H)-quinazolinone
Purity: ≥98% (HPLC)
Datasheet
Citations (2)
Reviews
Literature

Biological Activity

Ghrelin receptor antagonist (GHS-R1a) (Ki = 17 nM). Displays no significant affinity for the motilin receptor (Ki = 6 μM). Blocks the effects of ghrelin on insulin secretion both in vivo and in vitro. Improves glucose homeostasis in vivo.

Compound Libraries

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Technical Data

M. Wt 445.96
Formula C24H28FN3O2.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 875258-85-8
PubChem ID 74889155
InChI Key QQGRMONBDBMLSP-FERBBOLQSA-N
Smiles O=C2C1=CC(OC4=CC=C(F)C=C4)=CC=C1N=C(C)N2C[C@@H]3CN(C(C)C)CCC3.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 44.6 100
water 44.6 100

Preparing Stock Solutions

The following data is based on the product molecular weight 445.96. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.24 mL 11.21 mL 22.42 mL
5 mM 0.45 mL 2.24 mL 4.48 mL
10 mM 0.22 mL 1.12 mL 2.24 mL
50 mM 0.04 mL 0.22 mL 0.45 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

Esler et al (2007) Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss. Endocrinology 148 5175 PMID: 17656463

Moran and Dailey (2009) Gut peptides: targets for antiobesity drug development? Endocrinology 150 2526 PMID: 19372201


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Keywords: YIL 781, YIL 781 supplier, YIL781, YIL, 781, hydrochloride, ghrelin, receptors, antagonists, GHS-R1a, GHSR, Ghrelin, Receptors, 3959, Tocris Bioscience

2 Citations for YIL 781

Citations are publications that use Tocris products. Selected citations for YIL 781 include:

Evron et al (2014) G Protein and β-arrestin signaling bias at the ghrelin receptor. J Biol Chem 289 33442 PMID: 25261469

Song et al (2013) Ghrelin modulates lateral amygdala neuronal firing and blocks acquisition for conditioned taste aversion. PLoS One 8 e65422 PMID: 23762368


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Literature in this Area

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