TAN 452

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Cat.No. 6729 - TAN 452 | C29H30N2O5 | CAS No. 892039-23-5
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)
Datasheet
Citations
Reviews
Literature (5)

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.

Select a batch to recalculate based on the batch molecular weight:
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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Citations for TAN 452

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