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Submit ReviewL-365,260
Description: Selective CCK2 antagonist
Chemical Name: N-[(3R)-2,3-Dihydro-1-methyl-2-oxo-5-phenyl-1H-1,4-benzodiazepin-3-yl]-N'-(3-methylphenyl)urea
Purity: ≥99% (HPLC)
Biological Activity for L-365,260
L-365,260 is a selective cholecystokinin receptor 2 (CCK2) antagonist (IC50 values are 2 and 280 nM at CCK2 and CCK1 receptors respectively) that is inactive at a range of other receptors including opiate, muscarinic acetylcholine, α- and β adrenergic, histamine, angiotensin and bradykinin receptors.
Technical Data for L-365,260
| M. Wt | 398.46 |
| Formula | C24H22N4O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 118101-09-0 |
| PubChem ID | 5311201 |
| InChI Key | KDFQABSFVYLGPM-QFIPXVFZSA-N |
| Smiles | O=C1[C@H](NC(NC4=CC=CC(C)=C4)=O)N=C(C3=CC=CC=C3)C2=C(C=CC=C2)N1C |
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 L-365,260
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.85 | 100 | |
| ethanol | 39.85 | 100 |
Preparing Stock Solutions for L-365,260
The following data is based on the product molecular weight 398.46. 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 | 2.51 mL | 12.55 mL | 25.1 mL |
| 5 mM | 0.5 mL | 2.51 mL | 5.02 mL |
| 10 mM | 0.25 mL | 1.25 mL | 2.51 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets for L-365,260
References for L-365,260
References are publications that support the biological activity of the product.
Kees et al (1989) Benzodiazepine gastrin and brain cholecystokinin receptor ligands: L-365,260. J.Med.Chem. 32 13 PMID: 2909725
Lotti and Chang (1989) A new potent and selective non-peptide gastrin antagonist and brain cholecystokinin receptor (CCK-B) ligand: L-365,260. Eur.J.Pharmacol. 162 273 PMID: 2721567
Chung et al (2009) Cholecystokinin action on layer 6b neurons in somatosensory cortex. Brain Res. 1282 10 PMID: 19497313
If you know of a relevant reference for L-365,260, please let us know.
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Keywords: L-365,260, L-365,260 supplier, Selective, CCK2, antagonists, Cholecystokinin2, Receptors, L365260, Receptor, 2767, Tocris Bioscience
1 Citation for L-365,260
Citations are publications that use Tocris products. Selected citations for L-365,260 include:
Wu et al (2014) Role of cholecystokinin in anorexia induction following oral exposure to the 8-ketotrichothecenes deoxynivalenol, 15-acetyldeoxynivalenol, 3-acetyldeoxynivalenol, fusarenon X, and nivalenol. Toxicol Sci 138 278 PMID: 24385417
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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.