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Submit ReviewGR 89696 fumarate
Description: Subtype-selective κ agonist
Chemical Name: 4-[(3,4-Dichlorophenyl)acetyl]-3-(1-pyrrolidinylmethyl)-1-piperazinecarboxylic acid methyl ester fumarate
Purity: ≥99% (HPLC)
Biological Activity
Highly potent and selective κ-opioid agonist (IC50 = 0.04 nM) that may be selective for the putative κ2 receptor. Anti-nociceptive and neuroprotective in vivo.
Compound Libraries
GR 89696 fumarate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 530.4 |
| Formula | C19H25Cl2N3O3.C4H4O4 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 126766-32-3 |
| PubChem ID | 6442840 |
| InChI Key | ABTNETSDXZBJTE-WLHGVMLRSA-N |
| Smiles | [H]OC(=O)\C=C\C(=O)O[H].COC(=O)N1CCN(C(CN2CCCC2)C1)C(=O)CC1=CC=C(Cl)C(Cl)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 13.26 | 25 with gentle warming | |
| DMSO | 53.04 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 530.4. Batch specific molecular weights may vary from batch to batch due to the degree 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 | 1.89 mL | 9.43 mL | 18.85 mL |
| 5 mM | 0.38 mL | 1.89 mL | 3.77 mL |
| 10 mM | 0.19 mL | 0.94 mL | 1.89 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.38 mL |
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References
References are publications that support the biological activity of the product.
Birch et al (1991) Neuroprotective actions of GR89696, a highly potent and selective κ-opioid receptor agonist. Br.J.Pharmacol. 103 1819 PMID: 1657267
Butelman et al (2001) GR89,696: a potent κ-opioid agonist with subtype selectivity in rhesus monkeys. J.Pharmacol.Exp.Ther. 298 1049 PMID: 11504802
Naylor et al (1993) A potent new class of κ-receptor agonist: 4-substituted 1-(arylacetyl)-2-[(dialkylamino)methyl]piperazines. J.Med.Chem. 36 2075 PMID: 8393489
If you know of a relevant reference for GR 89696 fumarate, please let us know.
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Keywords: GR 89696 fumarate, GR 89696 fumarate supplier, Subtype-selective, κ-opioid, kappa-opioid, agonists, KOP, Receptors, OP2, GR89696, fumarate, Kappa, Opioid, 1483, Tocris Bioscience
Citations for GR 89696 fumarate
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