Biological Activity
Potent and selective, nonpeptide CCK2 receptor antagonist (IC50 values are 2.8 and 1232 nM for CCK2 and CCK1 respectively) that displays negligible affinity at GABAA, benzodiazepine, substance P, neurotensin, opioid, bradykinin and 5-HT3 receptors (IC50 > 10 μM). Exhibits anxiolytic activity in elevated plus maze and social interaction tests and increases food intake in rats.
Technical Data
| M. Wt | 616.76 |
| Formula | C35H44N4O6 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 130285-87-9 |
| PubChem ID | 44385784 |
| InChI Key | NNTPEWZUKRSTMM-CFHPNWNBSA-N |
| Smiles | C[C@](NC(OC3C4(C)CCC(C(C)4C)C3)=O)(C(NC[C@@H]([C@]5=CC=CC=C5)NC(CCC(O)=O)=O)=O)CC2=CNC1=CC=CC=C12 |
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 | 61.68 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 616.76. 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 | 1.62 mL | 8.11 mL | 16.21 mL |
| 5 mM | 0.32 mL | 1.62 mL | 3.24 mL |
| 10 mM | 0.16 mL | 0.81 mL | 1.62 mL |
| 50 mM | 0.03 mL | 0.16 mL | 0.32 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Dorre and Smith (1998) CholecystokininB receptor antagonist increases food intake in rats. Physiol.Behav. 65 11 PMID: 9811359
Tsutsumi et al (1999) Suppression of conditioned fear by administration of CCKB receptor antagonist PD135158. Neuropeptides 33 483 PMID: 10657528
Hughes et al (1990) Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc.Natl.Acad.Sci.USA 87 6728 PMID:
Keywords: PD 135158, supplier, Potent, selective, CCK2, antagonists, Cholecystokinin2, Receptors, PD135158, CAM1028, CAM, 1028, CCK2, Receptor, CCK2, Receptor, Tocris Bioscience
