Biological Activity
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
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 39.85 | 100 | |
| ethanol | 39.85 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 398.46. 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 | 2.51 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
References
References are publications that support the products' biological activity.
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
Keywords: L-365,260, supplier, Selective, CCK2, antagonists, Cholecystokinin2, Receptors, L365260, CCK2, Receptor, CCK2, Receptor, Tocris Bioscience
