TAN 452

Pricing Availability   Qty
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 (2)

Biological Activity for TAN 452

TAN 452 is a 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 for TAN 452

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 for TAN 452

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 48.66 100
ethanol 48.66 100

Preparing Stock Solutions for TAN 452

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 for TAN 452

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

Citations for TAN 452

Citations are publications that use Tocris products.

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Reviews for TAN 452

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Peptides Involved in Appetite Modulation Scientific Review

Peptides Involved in Appetite Modulation Scientific Review

Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.

Addiction Poster

Addiction Poster

The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.