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Description: Potent and selective peripherally acting δ opioid antagonist; antianalgesic.
Chemical Name: Ethyl (4bS,8R,8aS,14bR)-7-(cyclopropylmethyl)-5,6,7,8,8a,9,14,14b-octahydro-1,8a-dihydroxy-4,8-methanobenzofuro[2,3-a]pyrido[4,3-b]carbazole-12-carboxylate
Purity: ≥98% (HPLC)
Biological Activity
Potent and selective peripherally acting δ opioid antagonist; Ki values are 0.47, 5.31 and 36.56 nM at hDOR, hKOR, and hMOR, respectively. Kb values are 0.21, 7.18 and 9.43 nM, respectively. Attenuates morphine-induced side effects in vivo. Antianalgesic.
Technical Data
| M. Wt | 486.56 |
| Formula | C29H30N2O5 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 892039-23-5 |
| PubChem ID | 57614240 |
| InChI Key | JOJGLAWHRDFWNQ-KFDULEKRSA-N |
| Smiles | [H][C@@]12OC3=C(C=CC4=C3[C@@]15CCN([C@](C4)([C@@]5(CC6=C2NC7=CC(C(OCC)=O)=CC=C67)O)[H])CC8CC8)O |
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 | |||
| DMSO | 48.66 | 100 | |
| ethanol | 48.66 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 486.56. 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 | 2.06 mL | 10.28 mL | 20.55 mL |
| 5 mM | 0.41 mL | 2.06 mL | 4.11 mL |
| 10 mM | 0.21 mL | 1.03 mL | 2.06 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.41 mL |
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References
References are publications that support the biological activity of the product.
Lattanzi et al (2018) In vitro and in vivo pharmacological activities of 14-O-phenylpropyloxymorphone, a potent mixed mu/delta/kappa-opioid receptor agonist with reduced constipation in mice. Front.Pharmacol. 9 10.3389/fphar.2018.0 PMID: 30233377
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Keywords: TAN 452, TAN 452 supplier, TAN452, Potent, selective, peripherally, acting, delta, opioid, antagonists, antagonism, antianalgesic, Delta, Opioid, Receptors, 6729, Tocris Bioscience
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