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Submit ReviewLY 225910
Description: Potent CCK2 antagonist
Chemical Name: 2-[2-(5-Bromo-1H-indol-3-yl)ethyl]-3-[3-(1-methylethoxy)phenyl]-4-(3H)-quinazoline
Biological Activity for LY 225910
LY 225910 is a potent CCK2 receptor antagonist (IC50 = 9.3 nM for inhibition of 125I-labeled CCK-8 sulfate binding at mouse brain membranes).
Licensing Information
Sold with the permission of Eli Lilly and Company.
Technical Data for LY 225910
| M. Wt | 502.41 |
| Formula | C27H24BrN3O2 |
| Storage | Desiccate at -20°C |
| CAS Number | 133040-77-4 |
| PubChem ID | 4355450 |
| InChI Key | KUECXUACQOYKNB-UHFFFAOYSA-N |
| Smiles | CC(C)OC1=CC=CC(=C1)N1C(CCC2=CNC3=CC=C(Br)C=C23)=NC2=C(C=CC=C2)C1=O |
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.
Solubility Data for LY 225910
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100 |
Preparing Stock Solutions for LY 225910
The following data is based on the product molecular weight 502.41. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 1.99 mL | 9.95 mL | 19.9 mL |
| 5 mM | 0.4 mL | 1.99 mL | 3.98 mL |
| 10 mM | 0.2 mL | 1 mL | 1.99 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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Product Datasheets for LY 225910
References for LY 225910
References are publications that support the biological activity of the product.
Suman-Chauhan et al (1996) The influence of guanyl nucleotide on agonist and antagonist affinity at guinea-pig CCK-B / gastrin receptors: binding studies using [3H]PD140376. Regul.Pept. 65 37 PMID: 8876034
Yu et al (1991) Quinazolinone cholecystokinin receptor ligands. J.Med.Chem. 34 1505 PMID: 2016728
If you know of a relevant reference for LY 225910, please let us know.
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Keywords: LY 225910, LY 225910 supplier, Potent, CCK2, antagonists, Cholecystokinin2, Receptors, LY225910, Receptor, 1018, Tocris Bioscience
3 Citations for LY 225910
Citations are publications that use Tocris products. Selected citations for LY 225910 include:
Seillier et al (2013) Phencyclidine-induced social withdrawal results from deficient stimulation of cannabinoid CB1 receptors: implications for schizophrenia. Neuropharmacology 38 1816 PMID: 23563893
Karson et al (2008) Cholecystokinin inhibits endocannabinoid-sensitive hippocampal IPSPs and stimulates others. J Card Fail 54 117 PMID: 17689570
Gallopin et al (2006) Cortical sources of CRF, NKB, and CCK and their effects on pyramidal cells in the neocortex. Neuropsychopharmacology 16 1440 PMID: 16339088
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.