Biological Activity
Selective κ/δ-opioid heterodimer receptor agonist (EC50 = 39.8, 112.5 and > 1000 nM for κ/δ, κ/μ and δ/μ respectively) that has no effect on opioid receptor homodimers (EC50 > 1000 nM). Displays tissue-specific analgesic effects in vitro.
Technical Data
| M. Wt | 544.48 |
| Formula | C27H29N5O3.2HCl |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| PubChem ID | 90488790 |
| InChI Key | OCMMBKYOHYNDPT-GXOQRFFGSA-N |
| Smiles | OC1=CC=C2CC([C@@]3(O)[C@@]4(CC5)C2=C1O[C@H]4C(NC6=C7C=CC(NC(N)=N)=C6)=C7C3)N5CC8CC8.Cl.Cl |
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 | 54.45 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 544.48. 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 | 1.84 mL | 9.18 mL | 18.37 mL |
| 5 mM | 0.37 mL | 1.84 mL | 3.67 mL |
| 10 mM | 0.18 mL | 0.92 mL | 1.84 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Sharma et al (2001) Transformation of a κ-opoid receptor antagonist to a κ-agonist by transfer of a guanidinium group from the 5' to 6' position of naltrindole. J.Med.Chem. 44 2073 PMID: 11405645
Waldhoer et al (2005) A heterodimer-selective agonist shows in vivo relevance of G protein-coupled receptor dimers. Proc.Natl.Acad.Sci.USA 102 9050 PMID:
Rozenfeld et al (2006) Heterodimers of G protein-coupled receptors as novel and distinct drug targets. Drug Discov.Today Ther.Strateg. 3 437 PMID:
Rives et al (2012) 6'-guanidinonaltrindole (6'-GNTI) is a G protein-biased κ-opioid receptor agonist that inhibits arrestin recruitment. J.Biol.Chem. 287 27050 PMID: 22736766
Keywords: 6'-GNTI dihydrochloride, supplier, Selective, kappa/δ-opioid, delta-opioid, κ-opioid, kappa-opioid, heterodimer, receptor, agonists, KOP, Receptors, OP2, DOP, OP1, 6'-Guanidinonaltrindole, dihydrochloride, Kappa, Opioid, Receptors, Delta, Opioid, Receptors, Kappa, Opioid, Receptors, Tocris Bioscience
