Biological Activity
Potent and selective nociceptin/orphanin FQ (NOP) receptor antagonist (pA2 = 7.75). Displays selectivity for NOP receptors over classical opioid receptors (pKi values are 8.65, 6.60, 6.14 and < 5 for NOP, μ-, κ-, and δ-opioid receptors respectively). Attenuates motor deficits in a rat model of Parkinson's Disease. Active in vivo.
Compound Libraries
Trap 101 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 434.02 |
| Formula | C24H35N3O2.HCl |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1216621-00-9 |
| PubChem ID | 56972178 |
| InChI Key | YEVMLMQAMCKVSC-UHFFFAOYSA-N |
| Smiles | Cl.CCN1C(=O)N(C2=CC=CC=C12)C1=C(CO)CN(CC2CCCCCCC2)CC1 |
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 | 21.7 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 434.02. 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 | 2.3 mL | 11.52 mL | 23.04 mL |
| 5 mM | 0.46 mL | 2.3 mL | 4.61 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Trapella et al (2006) Identification of an achiral analogue of J-113397 as potent nociceptin/orphanin FQ receptor antagonist. Bioorg.Med.Chem. 14 692 PMID: 16202610
Marti et al (2008) The novel nociceptin/orphanin FQ receptor antagonist Trap-101 alleviates experimental parkinsonism through inhibition of the nigro-thalamic pathway: positive interaction with L-DOPA. J.Neurochem. 107 1683 PMID: 19014386
Keywords: Trap 101, supplier, Potent, selective, NOP, antagonists, Nociceptin, Receptors, ORL1, OP4, Opioid, Trap101, Parkinsons, disease, antiparkinsons, active, in, vivo, NOP, Receptors, NOP, Receptors, Tocris Bioscience
