6'-GNTI dihydrochloride

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Cat.No. 2962 - 6'-GNTI dihydrochloride | C27H29N5O3.2HCl
Description: Selective κ/δ opioid heterodimer receptor agonist
Alternative Names: 6'-Guanidinonaltrindole dihydrochloride
Chemical Name: 6''-Guanidinyl-17-(cyclopropylmethyl)-6,7-dehydro-4,5a-epoxy-3,14-dihydroxy-6,7-2',3'-indolomorphinan dihydrochloride
Purity: ≥97% (HPLC)
Datasheet
Citations
Reviews
Literature

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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

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


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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

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