PD 135158

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Cat.No. 2608 - PD 135158 | C35H44N4O6 | CAS No. 130285-87-9
Description: Potent and selective CCK2 antagonist
Alternative Names: CAM 1028
Chemical Name: 4-[[(1R)-2-[[(2R)-3-(1H-Indol-3-yl)-2-methyl-1-oxo-2-[[[[(1S,2R,4S)-1,7,7-trimethylbicyclo[2.2.1]hept-2-yl]oxy]carbonyl]amino]propyl]amino]-1-phenylethyl]amino]-4-oxobutanoic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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:


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Keywords: PD 135158, supplier, Potent, selective, CCK2, antagonists, Cholecystokinin2, Receptors, PD135158, CAM1028, CAM, 1028, CCK2, Receptor, CCK2, Receptor, Tocris Bioscience

Citations for PD 135158

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